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Journal articles on the topic 'Thiadiazol'

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Published: 5 June 2025

Last updated: 15 July 2025

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Singh, S., and Amandeep Kaur. "SYNTHESIS AND ANTICANCER ACTIVITY OF NOVEL 2-BENZYL-6- (SUBSTITUTED PHENYL)-IMIDAZO[2,1-B] [1,3,4] THIADIAZOLE DERIVATIVES." INDIAN DRUGS 56, no. 04 (2019): 13–20. http://dx.doi.org/10.53879/id.56.04.11454.

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A new series of 2-benzyl-6-(substituted phenyl)-imidazo[2,1-b][1,3,4] thiadiazoles (S1-S8) was synthesized as potential anti-cancer agents. These compounds were evaluated for their anticancer activity against various cancer cell lines. The anticancer activity data reveals that the compounds S1 (2-benzyl- 6-phenylimidazo[2,1-b][1,3,4]thiadiazole) showed maximum growth inhibition against CNS cancer cell lines while the compounds S2 (2-benzyl-6-(4-chlorophenyl) imidazo[2,1-b][1,3,4] thiadiazole) and S3 (2-benzyl-6-(2,4-dichlorophenyl)imidazo[2,1-b][1,3,4] thiadiazole) showed maximum inhibition against leukemia cell lines. The compounds S5 (2-(2-benzylimidazo[2,1-b] [1,3,4]thiadiazol-6-yl) phenol) and S6 (4-(2-benzylimidazo[2,1-b][1,3,4] thiadiazol-6-yl)benzene-1,3-diol) showed maximum inhibition against renal cancer cell lines and the compound S7 (3-(2-benzylimidazo[2,1-b][1,3,4] thiadiazol-6-yl) benzenamine) was most active against non-small cell lung cancer cell lines.

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C., S. ANDOTRA, C. LANGER T., and KOTHA AMRITA. "Synthesis and Antifungal Activity of some Substituted 1,3,4-Thiadiazolo[3,2-a]-s-triazin-5-phenyl-7-thiones and Imidazo-[2, 1-b ]-1,3,4-thiadiazol-5-ones." Journal of Indian Chemical Society Vol. 74, Feb 1997 (1997): 125–27. https://doi.org/10.5281/zenodo.5875250.

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Department of Chemistry. University of Jammu, Jammu-180 004 Manuscript received 25 October !994. revised 4 July 1995, accepted 4 August 1995 2-Amino-5-aryl-substituted-1,3,4-thiadiazoles (1) have been refluxed with benzoyllsothiocyanate to get N-[5-aryl-substituted-1,3,4- thiadiazol-2-yl)-N-benzoyl thlonreas (1a). These on refluxing with PCI5 and POCI3 give 2-aryl-substituted-1,3,4-thiadiazolo[3,2-a]-s- triazin-5-phenyl-7-thiones (3). Compound 1 on refluxing with chloroacetic acid and anhydrous sodium acetate gives 2-substituted-arylimidazo[2,1-b ]-1,3,4-thiadiazoi-5-ones (2). The compounds have been screened for antifungal activities.

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Zhao, Yuxiang, Peter J. McCarthy, and Cyril Párkányi. "Synthesis and In Vitro Evaluation of Novel Acyclic and Cyclic Nucleoside Analogs with a Thiadiazole Ring." ISRN Organic Chemistry 2013 (March 5, 2013): 1–10. http://dx.doi.org/10.1155/2013/159164.

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The synthesis of six thiadiazole nucleoside analogs is reported: 5-diacetylamino-1,2,4-thiadiazol-3-one (1), 5-amino-2- (tetrahydrofuran-2-yl)-1,2,4-thiadiazol-3-one (2), 5-amino-3-[(2′-hydroxyethoxy)methyl]-1,3,4-thiadiazol-2-one (3), 5-amino-3-(4′-hydroxy-2′-hydroxymethyl-butyl)-1,3,4-thiadiazole-2-thione (4), (R)-5-amino-3-(2′,3′-dihydroxypropyl)-1,3,4-thiadiazole-2-thione (5), and (S)-5-amino-3-(2′,3′-dihydroxypropyl)-1,3,4-thiadiazole-2-thione (6). The synthesis, characterization, and properties of these new synthesized thiadiazole derivatives are discussed. A dimerization of 5-amino-3H-1,3,4-thiadiazole-2-thione (14) by sodium nitrite resulting in di-(5-amino-1,3,4-thiadiazol-2-yl) disulfide (19) is also reported. The preliminary in vitro evaluation of these newly synthesized compounds is discussed.

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A. Ameen, Husam, and Ahlam J. Qasir. "Synthesis and Preliminary Antimicrobial Study of 2-Amino-5-Mercapto-1,3,4-Thiadiazole Derivatives." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 21, no. 1 (2017): 98–104. http://dx.doi.org/10.31351/vol21iss1pp98-104.

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Nitrogen heterocycles are of a special interest because they constitute an important class of natural and non natural products, many of which exhibit useful biological activities.Among these nitrogen heterocycles are 1, 3, 4-thiadiazole containing compounds. The therapeutic effects of these derivatives have been well studied for a number of pathological conditions including inflammation, pain, or hypertension. Moreover, synthesis of thiadiazoles has attracted wide-spread attention due to their diverse applications as antibacterial, anticancer, antifungal anti-inflammatory and antidepressant agents.According to this informationâ€™s new derivatives of 1, 3, 4-thiadiazole were designed and synthesized and in the hope of having some activities as antibacterial and antifungal. These are:  4-(((5-mercapto-1,3,4-thiadiazol-2-yl)imino)methyl)-2-methoxyphenol. Tert-butyl (1- ((2- ((5- (methylsulfonyl) -1,3,4- thiadiazol-2-yl) amino) -2- oxoethyl)amino) -1-oxopropan - 2-yl) carbamate.  Key words: 1, 3, 4-thiadiazole, biological activity, peptides, Schiff base.

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Rakhmonov, R., Sh Sharipov, M. Odilzoda, B. Safarov, A. Kobilzoda, and A. Abdurakhmonov. "SYNTHESIS AND FUNCTIONALIZATION OF SOME PARA-R-PHENYLIMIDAZO[2,1-B][1,3,4]- THIADIAZOLE DERIVATIVES." East European Scientific Journal 1, no. 4(68) (2021): 54–61. http://dx.doi.org/10.31618/essa.2782-1994.2021.1.68.15.

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The article describes the synthesis of new modifications of derivatives of 6-phenyl-, 6-piodophenyl- and 6-p-bromophenylimidazo[2,1-b][1,3,4]-thiadiazoles - N -((6-(4-iodophenyl)-2-R-imidazo[2,1-b][1,3,4]-thiadiazol-5-yl)methyl)-alkyl/ heterylamine based on the Mannich reaction, bromination 2((ethylsulfonyl)methyl)-6-phenylimidazo[2,1-b][1,3,4]-thiadiazole and the structure of the resulting compounds was established on the basis of IR spectroscopy. It was shown that the presence of substituents at the 2-nd position of the thiadiazole fragment and substituents at the 5th and 6th positions of the imidazole fragment of this heterocycle cause the appearance of a nonequivalent absorption band in the imidazo-thiadiazole fragment.

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Ardan, Bohdan, Vasyl Kinzhybalo, Yurii Slyvka, et al. "Ligand-forced dimerization of copper(I)–olefin complexes bearing a 1,3,4-thiadiazole core." Acta Crystallographica Section C Structural Chemistry 73, no. 1 (2017): 36–46. http://dx.doi.org/10.1107/s2053229616018751.

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As an important class of heterocyclic compounds, 1,3,4-thiadiazoles have a broad range of potential applications in medicine, agriculture and materials chemistry, and were found to be excellent precursors for the crystal engineering of organometallic materials. The coordinating behaviour of allyl derivatives of 1,3,4-thiadiazoles with respect to transition metal ions has been little studied. Five new crystalline copper(I) π-complexes have been obtained by means of an alternating current electrochemical technique and have been characterized by single-crystal X-ray diffraction and IR spectroscopy. The compounds are bis[μ-5-methyl-N-(prop-2-en-1-yl)-1,3,4-thiadiazol-2-amine]bis[nitratocopper(I)], [Cu2(NO3)2(C6H9N3S)2], (1), bis[μ-5-methyl-N-(prop-2-en-1-yl)-1,3,4-thiadiazol-2-amine]bis[(tetrafluoroborato)copper(I)], [Cu2(BF4)2(C6H9N3S)2], (2), μ-aqua-bis{μ-5-[(prop-2-en-1-yl)sulfanyl]-1,3,4-thiadiazol-2-amine}bis[nitratocopper(I)], [Cu2(NO3)2(C5H7N3S2)2(H2O)], (3), μ-aqua-(hexafluorosilicato)bis{μ-5-[(prop-2-en-1-yl)sulfanyl]-1,3,4-thiadiazol-2-amine}dicopper(I)–acetonitrile–water (2/1/4), [Cu2(SiF6)(C5H7N3S2)2(H2O)]·0.5CH3CN·2H2O, (4), and μ-benzenesulfonato-bis{μ-5-[(prop-2-en-1-yl)sulfanyl]-1,3,4-thiadiazol-2-amine}dicopper(I) benzenesulfonate–methanol–water (1/1/1), [Cu2(C6H5O3S)(C5H7N3S2)2](C6H5O3S)·CH3OH·H2O, (5). The structure of the ligand 5-methyl-N-(prop-2-en-1-yl)-1,3,4-thiadiazol-2-amine (Mepeta), C6H9N3S, was also structurally characterized. BothMepetaand 5-[(prop-2-en-1-yl)sulfanyl]-1,3,4-thiadiazol-2-amine (Pesta) (denotedL) reveal a strong tendency to form dimeric {Cu2L2}2+fragments, being attached to the metal atom in a chelating–bridging modeviatwo thiadiazole N atoms and an allylic C=C bond. Flexibility of the {Cu2(Pesta)2}2+unit allows the CuIatom site to be split into two positions with different metal-coordination environments, thus enabling the competitive participation of different molecules in bonding to the metal centre. ThePestaligand in (4) allows the CuIatom to vary between water O-atom and hexafluorosilicate F-atom coordination, resulting in the rare case of a direct CuI...FSiF52−interaction. Extensive three-dimensional hydrogen-bonding patterns are formed in the reported crystal structures. Complex (5) should be considered as the first known example of a CuI(C6H5SO3) coordination compound. To determine the hydrogen-bond interactions in the structures of (1) and (2), a Hirshfeld surface analysis has been performed.

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Zain Alabdeen, Khalid. "The Activity of 1,3,4 Thiadiazole Derivatives on the Soluble Oils." Journal of Petroleum Research and Studies 2, no. 1 (2021): 59–88. http://dx.doi.org/10.52716/jprs.v2i1.34.

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That Thiadiazoles derivative is biologically active as antimicrobial agents in cooling fluids. Derivatives of 1, 3, 4- thiadiazole have prepared:  2-amino-3-[(2-amino-1, 3, 4-thiadiazol-5-yl) dithio] propanoic acid. 2-(2-Carbethoxyamino-1, 3, 4-thiadiazol-5-yl)-thio acetic acid. [(5-amino-1,3,4-thiadiazol-2-yl) dithio] acetic acid  The synthesized compounds have been used as antimicrobial against the microorganisms which have been found in the cooling fluid of industrial purposes by using media culture the results showed that the compounds 1 and 3 are relatively highly active in killing bacteria from the compound 2. The pH of the cooling fluid samples had been measured after the addition of salt media as well as the inhibitors (1,2,3) the results of pH measurement revealed that the compounds 1,2 and 3 exhibit high activity to inhibit the growth of bacteria. The turbidity for such media and inhibitors has also been measured and the results indicated that 1,2 and 3 have given low turbidity to inhibit the bacteria or the microorganisms that grow in the cooling fluid.

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Pavlova, V. V., P. V. Zadorozhnii, V. V. Kiselev, A. V. Kharchenko, and O. V. Okhtina. "Modeling of new potential inhibitors of dihydrofolate reductase based on 1,3,4-thiadiazole amidoalkyl derivatives." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 5 (October 2023): 91–97. http://dx.doi.org/10.32434/0321-4095-2023-150-5-91-97.

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Derivatives of 1,3,4-thiadiazole are very important for medical chemistry and pharmacy as potential drug substances. In this work, we carried out molecular docking studies of amidoalkyl derivatives of 1,3,4-thiadiazole: N-(2,2,2-trichloro-1-((5-aryl-1,3,4-thiadiazol-2-yl)amino)ethyl)carboxamides and N-(2,2,2-trichloro-1-((5-(arylamino)-1,3,4-thiadiazol-2-yl)amino)ethyl)carboxamides with dihydrofolate reductase (DHFR). The AutoDock Vina program based on the PyRx 0.8 platform was used for docking. Before docking, the enzyme structure (PDB ID: 1DLS) was prepared using the Chimera 1.14 program, and the structures of potential inhibitors and reference preparations were optimized by the PM3 method in the ArgusLab 4.0.1 program. According to the results of molecular docking, the analyzed compounds effectively interact with the active site of DHFR. It is shown that the introduction of an NH group between the 1,3,4-thiadiazole and aromatic rings leads to stronger binding of ligands to DHFR. Based on the results of molecular docking, the following hit compounds were selected: 4-methyl-N-(2,2,2-trichloro-1-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)amino)ethyl)benzamide and 4-methyl-N-(2,2,2-trichloro-1-((5-(p-tolylamino)-1,3,4-thiadiazol-2-yl)amino)ethyl)benzamide, which are superior to the reference compounds according to the strength of the formed complex.

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Shein, Anatoliy B., Mariya D. Plotnikova, and Alexander E. Rubtsov. "PROTECTIVE PROPERTIES OF SOME THIADIAZOLE DERIVATIVES IN SULFURIC ACID SOLUTIONS." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENII KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 62, no. 7 (2019): 123–29. http://dx.doi.org/10.6060/ivkkt.20196207.5968.

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The work presents the results of the study of some thiadiazole derivatives as corrosion inhibitors for mild steel in 5-20% H2SO4. Gravimetric tests and electrochemical studies were performed on low-carbon steel St3 at ambient temperature. The exposure time of the samples was 24 h. Polarization curves were obtained by potentiodynamic method (v = 1 mV/s) in a three-electrode cell, using the SOLARTRON 1280 C electrochemical measuring complex. The following thiadiazole derivatives were studied: (E)-N,N-dimethyl-4-{[(5-phenyl-1,3,4-thiadiazol-2-yl)imino]methyl}aniline, (E)-5-{[4-(dimethylamino)benzylidene]amino}-1,3,4-thiadiazol-2-thiol, (E)-4-{[(5-(furan-2-yl)-1,3,4-thiadiazol-2-yl)imino]methyl}-N,N-dimethylaniline, N-(1,3,4-thiadiazol-2-yl)acetamide. It was established that the studied compounds at a concentration of 0.1 – 0.2 g/l show a good protective effect. The best result is given by (E)-5-{[4- (dimethylamino)benzylidene]amino}-1,3,4-thiadiazol-2-thiol with a protective effect Z more than 90%. The introduction of the benzene ring and the furan fragment into the molecules of the compounds under study leads to a decrease in their protective action as compared with the thiol group. With the help of electrochemical studies it was shown that the compounds studied are inhibitors of a mixed (cathodic-anodic) type, but to a greater extent they reduced the rate of the cathodic process. The results of the work indicate the promise of searching for potential acid corrosion inhibitors in a series of thiadiazole derivatives and the development of inhibiting compositions based on them.

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Journal, Baghdad Science. "SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME (2-AMINO-5-THIOL-1, 3, 4-THIADIAZOLE DERIVATIVES." Baghdad Science Journal 4, no. 1 (2007): 89–94. http://dx.doi.org/10.21123/bsj.4.1.89-94.

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Five derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4-thiadiazole, compound E: 2- amino-5-(2-Propanylthio)-1,3,4-thiadiazol) and compound F:2(o-chlorobenzylamino)-5-(2-propanyl thio)-1,3,4 thiadiazol. All prepared compounds were diagnosed by (IR) and (UV) Spectroscopy. All of those compounds were screened for their anti-microbial activity in vitro. The results show that most of the compounds A, B, C exhibited moderate to good activity against Gram-positive bacteria and the same compound exhibit low to moderate activity on most gram-negative bacteria under study. Finally, compound E and F had little or no effect organism.

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Drapak, І. V. "Synthesis, diuretic activity research and QSAR-analysis of N-(1,3,4-tiadiazol-2-il)substituted amides of alkanecarboxylic acids." Farmatsevtychnyi zhurnal, no. 2 (May 10, 2019): 55–65. http://dx.doi.org/10.32352/0367-3057.2.19.06.

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Diuretics are effective drugs that are widely used in medicine, but have unwanted side effects. The derivative of thiadiazole – acetozolamide is a known diuretic. Therefore, the search for diuretics in this series and the establishment of quantitative «structure–activity» (QSAR) dependencies is appropriate. The aim of the work was to synthesis N-(1,3,4-thiadiazol-2-yl)substituted alkanes of alkanecarboxylic acids, study their diuretic activity, and QSAR analysis. The objects of the study were N-(1,3,4-thiadiazol-2-yl)substituted alkanes of alkanecarboxylic acids, obtained by the interaction of 2-amino-5-alkyl-1,3,4-thiadiazole with the corresponding acylchlorides. Investigation of diuretic activity of synthesized compounds was carried out by the method of Berchin. Hyper-Chem and BuildQSAR software were used for calculation of molecular descriptors and QSAR-models. Synthesis of 12 N-(1,3,4-thiadiazol-2-yl)substituted amides of alkanecarboxylic acids, the structure of which was confirmed by PMR spectroscopy and elemental analysis. Studies of diuretic activity showed that the synthesized compounds had pronounced diuretic properties, and some of them according to activity indicators were approaching or exceeding comparative preparations. Compound N-(5-methyl-[1,3,4]thiadiazol-2-yl) propionamide showed the best diuretic effect: increased daily diuresis in white rats, in comparison with intact control, in 2.47 times (p ≤ 0,001), in comparison with hydrochlorothiazide was in 1,6 times and acetazolamide was 1,75 times. The calculation of the molecular descriptors of N-(1,3,4-thiadiazol-2-yl)substituted amides of alkanecarboxylic acids was conducted. Based on the calculated values of molecular descriptors and diuretic activity values of 12 synthesized compounds, a QSAR analysis was performed. Analysis of structure-diuretic activity showed the greatest influence of lipophilicity, energy parameters, spatial structure and size of the molecule. Moreover, diuretic activity increases with increasing logP, decreasing the refractive, volume and area of the molecule, increasing the energy of the higher occupied molecular orbital. Increasing the charge on the Sulfur atom of the thiadiazole ring and the Оxygen atom of the carbonyl group, reducing the angle between the Sulfur atoms, the Nitrogen of the amide group and the Oxygen, and increasing the angle between the Nitrogene atoms of the thiadiazole ring, the Oxygen and the Nitrogen of the amide group, also increases diuretic activity. The results of the diuretic activity of the synthesized compounds N-(1,3,4-thiadiazol-2-yl)substituted amides of alkanecarboxylic acids show the potential for the search for diuretic agents among 1,3,4-thiadiazole derivatives. The resulting QSAR models will be used to modelling and prediction the activity of new potential diuretics.

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Aggarwal, Navidha, and Sandeep Jain. "A Synthetic Approach, Characterization and Biological Evaluation of Novel 5-(Arylidene)-2-(5-methyl-1,3,4-thiadiazol-2-ylimino)thiazolidin-4-one Derivatives." Asian Journal of Chemistry 33, no. 7 (2021): 1530–36. http://dx.doi.org/10.14233/ajchem.2021.23203.

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The extensive biological potential of thiazolidin-4-one and 1,3,4-thiadiazole moieties, the novel string of 5-(arylidene)-2-(5-methyl-1,3,4-thiadiazol-2-ylimino)thiazolidin-4-one has been synthesized and characterized. The synthesized derivatives were screened for antimicrobial potential using serial tube dilution method. The results showed that all the synthesized compounds have significant biological activity against the microorganisms being tested. The antimicrobial activity of the compounds TA2, TA3, TA4, TA9, TA10 and TA20 against the tested microbial strains was promising. Compound TA4 (2-((5-methyl-1,3,4-thiadiazol-2-yl)imino)-5-(4-nitrobenzylidene)- thiazolidin-4-one) and TA2 (5-(4-chlorobenzylidene)-2-((5-methyl-1,3,4-thiadiazol-2-yl)imino)thiazolidin-4-one) showed promising antimicrobial activity against microbial strains. Compound TA9 (5-(4-(benzyloxy)benzylidene)-2-((5-methyl-1,3,4-thiadiazol-2-yl)imino)thiazolidin-4-one) was found to be the most effective towards B. subtilis. Compound TA10 (5-(3,4-dimethoxybenzylidene)-2-((5- methyl-1,3,4-thiadiazol-2-yl)imino)thiazolidin-4-one) was discovered to be the most potent against the Gram-negative bacteria. Compounds TA3 (5-(4-bromobenzylidene)-2-((5-methyl-1,3,4-thiadiazol- 2-yl)imino)thiazolidin-4-one) and TA20 (5-(2-bromobenzylidene)-2-((5-methyl-1,3,4-thiadiazol-2- yl)imino)thiazolidin-4-one) were the most effective compounds against the fungal strain.

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Ammar Ferman Abbood. "Synthesis, Characterization and Molecular Docking Study of New 1,3,4-Thiadiazole Derivatives." Journal of Wasit for Science and Medicine 17, no. 3 (2024): 26–38. http://dx.doi.org/10.31185/jwsm.503.

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In this study, a series of 5-(5-{(Z)-[(4-R1)methylidene]amino}-1,3,4-thiadiazol-2-yl)benzene-1,2,3-triol (L1-3), and 4-(5-{(Z)-[(4-R1)methylidene]amino}-1,3,4-thiadiazol-2-yl)benzene-1,2-diol (L4-6) compounds were synthesized, where R1 = 4-Nitro, 4-bromo, 4-chloro. The reaction between benzoic acid derivatives and hydrazinecarbothioamide in the basic medium gave the intended products with high yield and purity. The preparation of the compounds was confirmed by spectroscopic measurements in addition to physical properties. The biological properties of the prepared compounds were studied by molecular docking. The binding interaction between the new synthesized derivatives of 1,3,4-thiadiazole and the target, ADP-sugar pyrophosphatase, was studied. One of these 1,3,4-thiadiazole derivatives, 5-(5-{(Z)-[(4-nitrophenyl)methylidene]amino}-1,3,4-thiadiazol-2-yl)benzene-1,2,3-triol (L3) showed a high binding and coordination with its target. Molecular docking showed a docking score = −8.9 kcal/mol and MM-GBSA = −31.5 kcal/mol. The molecular docking estimation for the (L3) compound exhibited that four hydrogen bonds were created with NUDT5 Gene.

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Saeed, Ban M., Shaker A. Al-Jadaan, Rawa’a A. Kushaish, and Basil A. Abbas. "Antimicrobial activity, minimum inhibitory concentration and cytotoxicity of thiadiazol compound." Romanian Journal of Infectious Diseases 27, no. 1 (2024): 22–27. http://dx.doi.org/10.37897/rjid.2024.1.4.

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Aim. This study aims to investigate the biological activity and cytotoxicity of the prepared thiadiazole derivative compound. Methods. A thiadiazol chemical, 4-[5-amino 1,3,4-thiadiazole-2-yl] phenol, was prepared by reacting 2.762 grams (0.01 moles) of 4-hydroxybenzoic acid with 1.822 grams (0.01 moles) of thiosemicarbazide. The prepared thiadiazole antimicrobial activity was tested at concentrations of 30, 50, 80, and 100 mg/mL against Escherichia coli, Pseudomonas, Bacillus cereus, and Staphylococcus epidermidis. Results. The thiadiazole chemical compound was prepared and tested against several bacterial species. The minimum inhibitory concentration (MIC) for Escherichia coli, Bacillus cereus, and Staphylococcus epidermidis was 0.8 mg/mL. Pseudomonas was unaffected by this substance. Investigations were made into the cytotoxicity activities. When the concentration was less than 0.01 mg/mL, it was discovered that the produced thiadiazol also had no impact on the red blood cell. Conclusion. The results revealed that the thiadiazole chemical compound had strong antibacterial activity against some of the pathogenic bacteria. This means that the chemical compound can be used as a narrow spectrum antibiotic.

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Yu, Lu, Lingling Xiao, Pei Li, Jiyan Chi, Jie Li, and Shuming Tan. "Synthesis and Bioactivity Evaluation of Novel Thiochroman-4-One Derivatives Incorporating Carboxamide and 1, 3, 4-Thiadiazole Thioether Moieties." Journal of Chemistry 2022 (February 26, 2022): 1–7. http://dx.doi.org/10.1155/2022/5354088.

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A series of novel thiochroman-4-one derivatives incorporating carboxamide and 1, 3, 4-thiadiazole thioether moieties were synthesized. Bioassay results indicated that the EC50 values of compound 6-chloro-N-(5-(methylthio)-1, 3, 4-thiadiazol-2-yl)-4-oxothiochromane-2-carboxamide (5a) against Xanthomonas oryzae pv. Oryzae (Xoo) and Xanthomonas axonopodis pv. Citri (Xac) were 24 and 30 μg/mL, respectively, which were even better than those of bismerthiazol and thiadiazole copper. Meanwhile, compound 6-methyl-4-oxo-N-(5-(propylthio)-1, 3, 4-thiadiazol-2-yl)thiochromane-2-carboxamide (5m) showed a better antifungal activity against Botrytis cinerea (B. cinerea), with an inhibition rate of 69%, than carbendazim. As far as we know, this is the first report on the antibacterial and antifungal activities of this series of novel thiochroman-4-one derivatives incorporating carboxamide and 1, 3, 4-thiadiazole thioether moieties.

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Kokovina, Tatiana S., Svyatoslav Y. Gadomsky, Alexei A. Terentiev, and Nataliya A. Sanina. "A Novel Approach to the Synthesis of 1,3,4-Thiadiazole-2-amine Derivatives." Molecules 26, no. 17 (2021): 5159. http://dx.doi.org/10.3390/molecules26175159.

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The main purpose of the study was the development of a new method for synthesis of 1,3,4-thiadiazol-2-amine derivatives in a one-pot manner using the reaction between a thiosemicarbazide and carboxylic acid without toxic additives such as POCl3 or SOCl2. The reaction was investigated in the presence of polyphosphate ester (PPE). It was found that, in the presence of PPE, the reaction between the thiosemicarbazide and carboxylic acid proceeds in one-pot through three steps with the formation of corresponding 2-amino-1,3,4-thiadiazole. Using the developed approach five, 2-amino-1,3,4-thiadiazoles were synthesized. The structures of all compounds were proven by mass spectrometry, IR, and NMR spectroscopies.

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Toshmurodov, Turdibek, Abdukhakim Ziyaev, Sobirdjan Sasmakov, et al. "Amidoalkylation of heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]- 2'-chloroacetamide and antimicrobial activity of derivatives." Current Chemistry Letters 10, no. 4 (2021): 427–34. http://dx.doi.org/10.5267/j.ccl.2021.5.002.

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Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).

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JOHNSON, REEJA, JOBY THOMAS KAKKASSERY, Vinod Raphael Palayoor, Ragi Kooliyat, and Vidhya Thomas Kannanaikkal. "Experimental and Theoretical Investigations on the Corrosion Inhibition action of Thiadiazole Derivatives on Carbon Steel in 1M HCl medium." Oriental Journal Of Chemistry 36, no. 6 (2020): 1179–88. http://dx.doi.org/10.13005/ojc/360624.

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Novel thiadiazole derivatives of Schiff bases namely (E)-N-(anthracen-9-ylmethylene)-5-(4-nitrophenyl)-1,3,4-thiadiazol-2-amine (A9CNPTDA) and N-(anthracen-9(10H)-ylidene)-5-(4-nitrophenyl)-1,3,4-thiadiazol-2-amine (ANNPTDA) were synthesized, characterized and corrosion inhibition behaviour, as well as the mechanism of inhibition were investigated by different monitoring techniques like gravimetric measurements, electrochemical impedance spectroscopy, potentiodynamic polarization, quantum chemical and SEM studies. Both of the thiadiazole derivatives showed excellent corrosion inhibitor action on carbon Steel in acid medium. A9CNPTDA exhibited highest inhibition efficiency of 98.04% at 1mM concentration while ANNPTDA showed a maximum of 95.32%. In HCl medium, both derivatives obeyed Langmuir adsorption isotherm and thermodynamic parameters (Kads, ΔG0ads) were calculated. An acceptable relationship was observed between the results of quantum chemical calculations and other corrosion monitoring analysis.

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D., K. Raikwar, K. Srivastava S., and D. Srivastava S. "Synthesis of some new arylidenes-substituted phenyl-1,3,4-thiadiazol-4-oxothiazolidines : Antimicrobial and diuretic activities." Journal of Indian Chemical Society Vol. 85, Jan 2008 (2008): 78–84. https://doi.org/10.5281/zenodo.5808560.

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Synthetic Organic Chemistry Laboratory, Department of Chemistry, Dr. H. S. Gour University, Sagar-470 003, Madhya Pradesh, India E-mail: professorsks@rediffmail.com Manuscript received 9 January 2007, revised 21 August 2007, accepted 16 October 2007 A series of new [2-(substituted aryl)-3-{5-(substituted phenyl)-1,3,4-thiadiazol}]-4-oxo-thiazolidines, 3(ao) have been synthesized via the condensation of 5-(substituted phenyl)-2-(2-substituted benzylidene amino)-1,3,4- thiadiazoles, 2(a-o) with thioglycolic acid. The compounds 2(a-o) were synthesized from 5-(substituted phenyl)-2- amino-1,3,4-thiadiazole, l(a-c) with various aromatic aldehydes which itself was prepared from substituted aromalic acid(s) using thiosemicarbazide. The compounds 3(a-o) on treatment with various aromatic aldehydes afforded [5- (substituted arylidenes)-2-(substituted aryl)-3-{ 5-(substituted phenyl)-1 ,3,4-thiadiazol }1-4-oxo-thiazolidines, 4(a-o). The structures of all the synthesized compounds have been determined by spectral and chemical methods. The compounds 2, 3 and 4 were screened for their antifungal and antibacterial activities against E. coli, S. typhimurium and B. subtilis bacteria and R. oryzae, C. albicans and A. niger fungi and diuretic activity on adult male rats.

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Kumar, Deepak. "Synthesis and Characterization of Thiadiazole Pyrazolene Anthranilic Acid Derivatives as Potent Anti-inflammatory Agents." Asian Journal of Organic & Medicinal Chemistry 7, no. 1 (2022): 84–91. http://dx.doi.org/10.14233/ajomc.2022.ajomc-p366.

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Several new substituted thiadiazole pyrazolene anthranilic acid derivatives were synthesized. These compounds also evaluated for their anti-inflammatory and analgesic activities. Compound 2-((5-(3- (2,6-dichloro)acrylamido)-1,3,4-thiadiazol-2-yl)methyl amino)-benzoic acid (5b) and 2-((5-(1-acetyl- 5-(2,6-dichloro)-4,5-dihydro-1H-pyrazol-3-ylamino)-1,3,4-thiadiazol-2-yl)methyl amino)benzoic acid (6b) were found to be most active compounds of this series, which exhibits 38.10 & 48.50% anti-inflammatory activity while, 36.24 & 40.10 % analgesic activity, respectively. The structures of all the compounds were characterized by analytical data, IR, 1H NMR and mass spectrometry.

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Zhivotova, T. S., R. E. Bakirova, S. D. Fazylov, S. K. Kabieva, and T. V. Kryazheva. "Synthesis and Biological Activity of 2,5-Bisubstituted Derivatives of 1,3,4-Thiadiazol-2,5-dithiol." Journal of Chemistry 2013 (2013): 1–4. http://dx.doi.org/10.1155/2013/635079.

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By reaction of 1,3,4-thiadiazol-2,5-dithiol with different organohalogens, chlorides of carboxylic acids, acrylic acid derivatives, alkaloids, and secondary amines, various derivatives of 2,5-bi-substituted 1,3,4-thiadiazole were synthesized, and biological properties of some of them were studied.

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NizamMohideen, M., S. Syed Abuthahir, V. Viswanathan, D. Velmurugan, and M. Karthik Ananth. "The crystal structures and Hirshfeld surface analyses of four 3,5-diacetyl-2-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yl derivatives." Acta Crystallographica Section E Crystallographic Communications 75, no. 10 (2019): 1436–44. http://dx.doi.org/10.1107/s2056989019011915.

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The title compounds, 4-(5-acetamido-3-acetyl-2-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)phenyl benzoate, C20H19N3O4S (I), 4-(5-acetamido-3-acetyl-2-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)phenyl isobutyrate 0.25-hydrate, C17H21N3O4S·0.25H2O (II), 4-(5-acetamido-3-acetyl-2-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)phenyl propionate, C16H19N3O4S (III) and 4-(5-acetamido-3-acetyl-2-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yl)phenyl cinnamate chloroform hemisolvate, C22H21N3O4S·0.5CHCl3 (IV), all crystallize with two independent molecules (A and B) in the asymmetric unit in the triclinic P\overline{1} space group. Compound II crystallizes as a quaterhydrate, while compound IV crystallizes as a chloroform hemisolvate. In compounds I, II, III (molecules A and B) and IV (molecule A) the five-membered thiadiazole ring adopts an envelope conformation, with the tetrasubstituted C atom as the flap. In molecule B of IV this ring is flat (r.m.s. deviation 0.044 Å). The central benzene ring is in general almost normal to the mean plane of the thiadiazole ring in each molecule, with dihedral angles ranging from 75.8 (1) to 85.5 (2)°. In the crystals of all four compounds, the A and B molecules are linked via strong N—H...O hydrogen bonds and generate centrosymmetric four-membered R 4 4(28) ring motifs. There are C—H...O hydrogen bonds present in the crystals of all four compounds, and in I and II there are also C—H...π interactions present. The intermolecular contacts in the crystals of all four compounds were analysed using Hirshfeld surface analysis and two-dimensional fingerprint plots.

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Joseph, Alex, Chaitanyakumar S. Shah, Suthar Sharad Kumar, et al. "Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones." Acta Pharmaceutica 63, no. 3 (2013): 397–408. http://dx.doi.org/10.2478/acph-2013-0028.

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Abstract A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC50 less than 150 μmol L-1. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 μmol L-1, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 μmol L-1.

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Susumu, Kimihiro, and Michael J. Therien. "Design of diethynyl porphyrin derivatives with high near infrared fluorescence quantum yields." Journal of Porphyrins and Phthalocyanines 19, no. 01-03 (2015): 205–18. http://dx.doi.org/10.1142/s1088424614501107.

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A design strategy for (porphinato)zinc-based fluorophores that possess large near infrared fluorescence quantum yields is described. These fluorophores are based on a (5,15-diethynylporphinato)zinc(II) framework and feature symmetric donor or acceptor units appended at the meso-ethynyl positions via benzo[c][1,2,5]thiadiazole moieties. These (5,15-bis(benzo[c][1′,2′,5′]thiadiazol-4′-ylethynyl)-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (4), (5,15-bis[4′-(N,N-dihexylamino) benzo[c][1′,2′,5′]thiadiazol-7′-ylethynyl]-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (5), (5,15-bis([7′-(4″-n-dodecyloxyphenylethynyl)benzo[c][1′,2′,5′]thiadiazol-4′-yl]ethynyl)-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (6), (5,15-bis([7′-([7″-(4″ ′-n-dodecyloxyphenyl)benzo[c][1″,2″,5″]thiadiazol-4″-yl]ethynyl)benzo[c][1′,2′,5′]thiadiazol-4′-yl]ethynyl)-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (7), 5,15-bis ([7′-(4″-N,N-dihexylaminophenylethynyl)benzo[c][1′,2′,5′]thiadiazol-4′-yl]ethynyl)-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (8), and (5,15-bis([7′-(4″-N,N-dihexylaminophenylethenyl)benzo[c][1′,2′,5′]thiadiazol-4′-yl]ethynyl)-10,20-bis[2′,6′-bis(3″,3″-dimethyl-1″-butyloxy)phenyl]porphinato)zinc(II) (9) chromophores possess red-shifted absorption and emission bands that range between 650 and 750 nm that bear distinct similarities to those of the chlorophylls and structurally related molecules. Interestingly, the measured radiative decay rate constants for these emitters track with the integrated oscillator strengths of their respective x-polarized Q-band absorptions, and thus define an unusual family of high quantum yield near infrared fluorophores in which emission intensity is governed by a simple Strickler–Berg dependence.

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Mali, Suraj N., Sudhir Sawant, Hemchandra K. Chaudhari, and Mustapha C. Mandewale. "In Silico Appraisal, Synthesis, Antibacterial Screening and DNA Cleavage for 1,2,5-thiadiazole Derivative." Current Computer-Aided Drug Design 15, no. 5 (2019): 445–55. http://dx.doi.org/10.2174/1573409915666190206142756.

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Background: : Thiadiazole not only acts as “hydrogen binding domain” and “two-electron donor system” but also as constrained pharmacophore. Methods:: The maleate salt of 2-((2-hydroxy-3-((4-morpholino-1, 2,5-thiadiazol-3-yl) oxy) propyl) amino)- 2-methylpropan-1-ol (TML-Hydroxy)(4) has been synthesized. This methodology involves preparation of 4-morpholino-1, 2,5-thiadiazol-3-ol by hydroxylation of 4-(4-chloro-1, 2,5-thiadiazol-3-yl) morpholine followed by condensation with 2-(chloromethyl) oxirane to afford 4-(4-(oxiran-2-ylmethoxy)-1,2,5-thiadiazol- 3-yl) morpholine. Oxirane ring of this compound was opened by treating with 2-amino-2-methyl propan-1- ol to afford the target compound TML-Hydroxy. Structures of the synthesized compounds have been elucidated by NMR, MASS, FTIR spectroscopy. Results: : The DSC study clearly showed that the compound 4-maleate salt is crystalline in nature. In vitro antibacterial inhibition and little potential for DNA cleavage of the compound 4 were explored. We extended our study to explore the inhibition mechanism by conducting molecular docking, ADMET and molecular dynamics analysis by using Schrödinger. The molecular docking for compound 4 showed better interactions with target 3IVX with docking score of -8.508 kcal/mol with respect to standard ciprofloxacin (docking score= -3.879 kcal/mol). TML-Hydroxy was obtained in silico as non-carcinogenic and non-AMES toxic with good percent human oral absorption profile (69.639%). TML-Hydroxy showed the moderate inhibition against Mycobacteria tuberculosis with MIC 25.00 μg/mL as well as moderate inhibition against S. aureus, Bacillus sps, K. Pneumoniae and E. coli species. Conclusion: : In view of the importance of the 1,2,5-thiadiazole moiety involved, this study would pave the way for future development of more effective analogs for applications in medicinal field.

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Moshafi, Hassan, Azadeh Yahya-Meymandi, Esmaeil Sadat-Ebrahimi, et al. "Synthesis and biological activity of 5-nitrofuran-containing (1,3,4-thiadiazol-2-yl)piperazine moieties as a new type of anti-Helicobacter pylori heterocycles." Journal of the Serbian Chemical Society 76, no. 2 (2011): 201–10. http://dx.doi.org/10.2298/jsc100324013m.

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In order to find new and potent drug candidates for the treatment of Helicobacter pylori infections? in this study attention was focused on the synthesis and anti-H. pylori activity of a series of 5-(5-nitrofuran-2- yl)-1,3,4-thiadiazoles containing piperazinyl functionality at the C-2 position of the 1,3,4-thiadiazole ring. The synthesis of 1-[5-(5-nitrofuran- 2-yl)-1,3,4-thiadiazol-2-yl]piperazine derivatives (3a-h) and pyrrolidine derivative 3i was achieved with a versatile and efficient synthetic route via 2-chloro-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazole. The inhibitory activity of the new derivatives 3a-i against twenty clinical H. pylori strains was evaluated by the disc diffusion method and compared with the commercially available standard drug metronidazole Resulting biological data indicated that most compounds exhibited strong inhibitory activity even at doses lower than 2 ?g disc-1 (average of inhibition zone >20 mm) while metronidazole had little or no growth inhibition at this dose. Compound 3c containing the N-benzoylpiperazin-1-yl moiety showed the most potent inhibitory activity.

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Khadgamala, N. Sridevi, V. Narasinga Rao, K. Apparao, B. V. Durgarao, B. S. Diwakar, and N. Krishna Rao. "CuI Promoted Efficient Synthesis and Antimicrobial Activity of Substituted 8,8-Dimethyl-5-phenyl-2-(pyrazin-2-yl)-5,7,8,9-tetrahydro-6H-[1,3,4]thiadiazolo[2,3-b]quinazolin-6-one." Asian Journal of Chemistry 36, no. 4 (2024): 895–900. http://dx.doi.org/10.14233/ajchem.2024.30890.

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In present study, an efficient synthesis of substituted 5,7,8,9-tetrahydro-6H-[1,3,4]thiadiazolo[2,3-b]quinazolin-6-one compounds promoted by CuI as catalyst was carried out. These derivatives were obtained from 1,3,4-thiadiazol-2-amine, dimedone and substituted aromatic aldehyde in presence of CuI in ethanol as solvent at 70 ºC. Initially, 1,3,4-thiadiazol-2-amine was synthesized from pyrazine-3- carboxylic acid reacted with thiosemicarbazide in the presence of 50% H2SO4 in acetonitrile at 70 ºC. All the newly obtained derivatives were evaluated by the spectroscopic techniques such as 1H NMR, 13C NMR and LCMS and structural determination of titled analogous were analyzed by elemental analysis. The antibacterial activities of the newly synthesized compounds were also screened.

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Gudim, Nikita S., Ekaterina A. Knyazeva, Natalia V. Obruchnikova, Oleg A. Rakitin, and Vadim V. Popov. "4-(7-Bromobenzo[d][1,2,3]thiadiazol-4-yl)morpholine." Molbank 2021, no. 2 (2021): M1202. http://dx.doi.org/10.3390/m1202.

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Dibromoderivatives of benzofused chalcogen-nitrogen heterocycles are important precursors in the synthesis of various photovoltaic materials. 4,7-Dibromobenzo[d][1,2,3]thiadiazole is a practically unexplored compound in this series. In this communication, it was shown that the nucleophilic substitution of 4,7-dibromobenzo[d][1,2,3]thiadiazole with morpholine gave selectively 4-substituted product—4-(7-bromobenzo[d][1,2,3]thiadiazol-4-yl)morpholine. The structure of the newly synthesized compound was established by means of elemental analysis, high resolution mass-spectrometry, 1H, 13C NMR, and IR spectroscopy, mass-spectrometry, and X-ray analysis.

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Makwane, Sunil, SD Srivastava, Rajiv Dua, and SK Srivastava. "Synthesis and Antimicrobial Activity of 4-Oxo-Thiazolidines and 5-Arylidene Derivatives of 2-Amino-5-Ethyl-1,3,4-Thiadiazole." Journal of Bangladesh Academy of Sciences 42, no. 2 (2018): 155–70. http://dx.doi.org/10.3329/jbas.v42i2.40042.

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A new series of 5-benzylidene-3-(5-ethyl-[1,3,4]thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones (3a-3m) were synthesized. The reaction of thioglycolic acid with benzylidene-(5-ethyl-[1,3,4] thiadiazol-2-yl)-amine 1a in the presence of anhydrous ZnCl2 afforded the new heterocyclic compounds 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazole-yl)-2-phenyl-thiazolidin-4-one, 2a. The latter product on treatment with several selected substituted aromatic aldehydes in the presence of sodium ethoxide underwent the Knoevenagel reaction to yield 5-benzylidene-3-(5-ethyl-[1,3,4] thiadiazol-2-yl)-2-phenyl-thiazolidin-4-ones, 3a-3m. The structures of the compounds were confirmed by IR, 1H-NMR, 13C-NMR and mass spectroscopy and by chemical analysis. All the above compounds were screened for their antimicrobial activity against some selected bacteria and fungi such as E. coli, B. Subtilis, and S. Typhi bacteria and A.niger, A. Flavus and F. oxisporium Fungi. Journal of Bangladesh Academy of Sciences, Vol. 42, No. 2, 155-170, 2018

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Wadhwa, Preeti, Tanpreet Kaur, and Anuj Sharma. "The first catalyst and solvent-free synthesis of 2-arylimidazo[2,1-b][1,3,4]thiadiazoles: a comparative assessment of greenness." RSC Advances 5, no. 55 (2015): 44353–60. http://dx.doi.org/10.1039/c5ra06747b.

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A one-pot, three-component, catalyst and solvent free synthesis of imidazo[2,1-b][1,3,4]thiadiazoles utilizing 5-aryl-1,3,4-thiadiazol-2-amines, aldehydes and isonitriles has been developed. The “greenness” was successfully evaluated within the ambits of green metrics.

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K, Vandana, Anoob Kumar K. I, Jisha Prems, Vidhya K. M, and Lal Prasanth M. L. "Characterization & Invitro Antioxidant Activity of 1, 3, 4 Thiadiazole Derivatives of Thiazolidinone." Saudi Journal of Medical and Pharmaceutical Sciences 11, no. 06 (2025): 452–61. https://doi.org/10.36348/sjmps.2025.v11i06.002.

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In view of the considerable importance of thiadiazoles and thiazolidinones, which are the core structures in a variety of pharmaceuticals with a broad spectrum of biological activity. Synthesis of series of potential biological active 1, 3, 4 thiadiazole linked 4 thiazolidinone derivatives were obtained via a multistep synthesis sequence with a simple and convenient approach by using substituted benzoic acids, which are expected to possess enhanced antioxidant activity based on the literature survey reports. In the present study the initial compound, 5-phenyl-1, 3, 4-thiadiazol-2-amine was treated with different substituted aromatic aldehydes to produce Schiff base. The resulting Schiff base were subjected to addition reactions with thioglycolic acid to form title compounds of 2-phenyl-3-(5-phenyl-1,3,4-thiadiazol-2-yl)-1,3-thiazolidin-4-one. The structure of the synthesized compounds was characterised by FT-IR, H1NMR and mass spectral analysis. The synthesized compounds were tested for antioxidant activities with standard drug using DPPH method. The results of this study revealed that, among the compound tested for antioxidant activity, TZD 5 and TZD 3 exhibited promising antioxidant activity with the IC50 value 27.50µM and 28.00µM while the value of reference compound, ascorbic acid 29.2µM. The antioxidant screening results indicate that exciting DPPH radical scavenging activity was observed in compounds (TZD 3 and TZD 5) in comparison with standard ascorbic acid. These results may also provide some significance guidance for the development of new class antioxidant.

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Smith, Graham, and Daniel E. Lynch. "Molecular cocrystals of 5-(4-bromophenyl)-1,3,4-thiadiazol-2-amine: hydrogen bonding in the structures of the 1:1 adduct with 2-(naphthalen-2-yloxy)acetic acid and the salt with 3,5-dinitrobenzoic acid." Acta Crystallographica Section C Crystal Structure Communications 69, no. 9 (2013): 1034–38. http://dx.doi.org/10.1107/s0108270113019665.

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The crystal structures of the anhydrous products from the interaction of 5-(4-bromophenyl)-1,3,4-thiadiazol-2-amine with 2-(naphthalen-2-yloxy)acetic acid,viz.the 1:1 adduct C8H6BrN3S·C12H10O3, (I), and with 3,5-dinitrobenzoic acid,viz.the salt 2-amino-5-(4-bromophenyl)-1,2,4-thiadiazol-3-ium 3,5-dinitrobenzoate, C8H7BrN3S+·C7H3N2O6−, (II), have been determined. In adduct (I), a heterodimer is formed through a cyclic hydrogen-bonding motif [graph setR22(8)], involving carboxylic acid–heteroatom O—H...N and amine–carboxylic acid N—H...O interactions. The heterodimers are essentially planar, with a thiadiazole-to-naphthalene ring dihedral angle of 15.9 (2)° and an intramolecular thiadiazole-to-benzene ring angle of 4.7 (2)°. An amine–heteroatom N—H...N hydrogen bond between the heterodimers generates a one-dimensional chain structure extending down [001]. Also present are weak benzene–benzene and naphthalene–naphthalene π–π stacking interactions down thebaxis [minimum ring-centroid separation = 3.936 (3) Å]. With salt (II), the cation–anion association is also through a cyclicR22(8) motif but involving duplex N—H...Ocarboxylatehydrogen bonds, giving a heterodimer that is close to planar [dihedral angles between the thiadiazole ring and the two benzene rings = 5.00 (16) (intra) and 7.23 (15)° (inter)]. A secondary centrosymmetric cyclic R_{4}^{2}(8) N—H...Ocarboxylatehydrogen-bonding association involving the second amino H atom generates a heterotetramer. Also present in the crystal structure are weak π–π interactions between thiadiazolium rings [minimum ring-centroid separation = 3.9466 (18) Å], as well as a short Br...Onitrointeraction [3.314 (4) Å]. The two structures reported here now provide a total of three crystallographically characterized examples of cocrystalline products from the interaction of 5-(4-bromophenyl)-1,3,4-thiadiazol-2-amine with carboxylic acids, of which only one involves proton transfer.

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Walek, Wolfgang, Christine Fieseler, Peter Schneider, and Gerhard W. Fischer. "Notizen: Trennung und biologische Wirksamkeit der Enantiomeren eines chiralen Thiadiazolylsulfoxides/Separation and Biological Activity of the Enantiomers of a Chiral Thiadiazolyl Sulfoxide." Zeitschrift für Naturforschung B 47, no. 4 (1992): 597–99. http://dx.doi.org/10.1515/znb-1992-0424.

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The enantiomers of the fungicidal and bactericidal (3-chloro-1,2,4-thiadiazol-5-yl)-(3´-chloro-1´,2´,4´-thiadiazoyl-5´-ylthiomethyl)-sulfoxide (2) have been separated by liquid chromatography on triacetylcellulose. Tested in a photometer assay on Torulopsis H 24 and Erwinia carotovorum (+)-2 and (-)-2 show practically the same activity and do not differ from the racemic mixture.

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Journal, Baghdad Science. "Synthesized azodyes of 2-amino-1, 3, 4- thiadiazole - 5 - thiol." Baghdad Science Journal 8, no. 2 (2011): 269–73. http://dx.doi.org/10.21123/bsj.8.2.269-273.

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Several azo dyes were synthesized through coupling reaetion of some substituted phenols and B.naphthol with diazonium salt of 2- amino-1,3-4- thiadiazol -5- thiol. All the synthesized compounds during this work were characterized using some speetral data (F.TIRand UV)andM.P . 2-[4 --Hydroxy napthyl-azo ] -1,3,4-Thiadiazol -5-Thiol • 2- [2-- hydroxy –4- NO2 – phenyl- azo]- 1,3,4 - Thiadiazol –5-Thiol. • 2- [3--Amino-4-Hydroxy phenyl –azo]-1,3,4 - Thiadiazol –5-Thiol. . • 2-[2--Amino-4-Hydroxy phenyl -azo]-1,3,4 - Thiadiazol –5-Thiol . • 2- [3--Amino-6- Hydroxy phenyl -azo]-1,3,4 - Thiadiazol –5-Thiol. • 2-[2-- Hydroxy- 5 – chloro – Pheny - azo]- 1,3,4 - Thiadiazol –5-Thiol . • 2- [4-- Hydroxy phenyl -azo] -1,3,4 - Thiadiazol –5-Thiol . • 2- [ 3-- Bromo – 6 -- Hydroxy - phenyl –1-azo] – 1,3,4, Thiadiazol –5-Thiol .

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Broumidis, Emmanouil, Samuel B. H. Patterson, Georgina M. Rosair, Panayiotis A. Koutentis, and Andreas S. Kalogirou. "2-Benzoyl-4-phenyl-1,2,5-thiadiazol-3(2H)-one 1,1-Dioxide." Molbank 2024, no. 1 (2024): M1774. http://dx.doi.org/10.3390/m1774.

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3,5-Diphenyl-4H-1,2,6-thiadiazin-4-one treated with meta-chloroperoxybenzoic acid undergoes an oxidative ring contraction to give 2-benzoyl-4-phenyl-1,2,5-thiadiazol-3(2H)-one 1,1-dioxide in a 29% yield, the structure of which is supported by single-crystal X-ray diffraction analysis and the available spectroscopic data.

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H., J. VIKANI, and PAREKH HANSA. "Studies on Thiadiazole Derivatives. Part-III. Preparation and Antimicrobial Activity of p,p -Bis(2-substituted-benzalamino/ benzoyl- amino/sulphonamido-1 ,3,4-thiadiazol-5- ylmethylamino)diphenyl Sulphones." Journal of Indian Chemical Society Vol. 67, Oct. 1990 (1990): 859–61. https://doi.org/10.5281/zenodo.6278954.

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Department of Chemistry, Saurashtra University, Rajkot-360 005 Manuscript received 8 December 1989, revised 18 June 1990, accepted 22 August 1990 Studies on Thiadiazole Derivatives. Part-III. Preparation and Antimicrobial Activity of p,p -Bis(2-substituted-benzalamino/benzoyl- amino/sulphonamido-1,3,4-thiadiazol-5- ylmethylamino)diphenyl Sulphones

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Malak, Sajid Ajit, Jamatsing Dabarsing Rajput, and Mustakim Sharif. "Design, synthesis, spectral analysis, and biological evaluation of Schiff bases with a 1,3,4-thiadiazole moiety as an effective inhibitor against bacterial and fungal strains." European Journal of Chemistry 14, no. 4 (2023): 466–72. http://dx.doi.org/10.5155/eurjchem.14.4.466-472.2468.

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Many distinct natural and pharmaceutical items include the well-known heterocyclic nucleus 1,3,4-thiadiazole. Ten Schiff bases of 1,3,4-thiadiazole derivatives have been synthesized using equimolar amounts of 5-styryl-1,3,4-thiadiazol-2-amine and substituted acetophenones in the catalytic amount of ethanol. The synthesized derivatives of Schiff's bases were characterized by FT-IR, 1H NMR, 13C NMR, and mass spectroscopy. The 1,3,4-thiadiazole Schiff’s bases (RM-1 to RM-10) were tested for their in vitro antimicrobial activity against Pseudomonas aeruginosa, Escherichia coli, Bacillus subtilis, Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus using the disc diffusion method. The 1,3,4-thiadiazole Schiff bases showed strong antibacterial activity against bacterial and fungal species, however, their activity was noticeably less effective than that of the evaluated conventional antibiotics.

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Ibrahim, Yusria R. "Synthesis of imidazo- and pyrazolothiadiazoles from dithiobiureas and dimethyl ethynedicarboxylate." Journal of Chemical Research 2009, no. 10 (2009): 602–6. http://dx.doi.org/10.3184/030823409x12510192920270.

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Microwave irradiation of 1-substituted-2, 5-dithiobiureas and 1, 6-disubstituted-2, 5-dithiobiureas with dimethyl ethynedicarboxylate gave methyl 2-{6-oxo-2-(substituted amino)imidazo-[2, 1- b][1, 3, 5]thiadiazol-5(6 H)-ylidene} acetate and methyl 7-oxo-1, 3-bis(substituted imino)-3, 7-dihydro-1 H-pyrazolo[1, 2- c][1, 3, 4]thiadiazole-5-carboxylate. Rationales for these transformations are presented.

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Kurteva, Vanya, Rusi Rusew, and Boris Shivachev. "4-Methyl-7-((2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethyl)thio)-coumarin." Molbank 2022, no. 4 (2022): M1491. http://dx.doi.org/10.3390/m1491.

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The novel compound 4-methyl-7-((2-((5-methyl-1,3,4-thiadiazol-2-yl)thio)ethyl)thio)-coumarin is obtained in good yield via a two-step protocol; that is, initial synthesis of the reagent 2-((2-chloroethyl)thio)-5-methyl-1,3,4-thiadiazole followed by alkylation of 7-mercapto-4-methylcoumarin. The product’s structure is assigned by 1D and 2D NMR experiments and is confirmed by single-crystal XRD.

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Vedika Dadlani, Pushpendra Tripathi, and Rakesh Somani. "Design, Molecular Docking and In-Silico Analysis of Novel thiadiazole-azetidinone hybrids as Potential Antitubercular Agents." International Journal of Research in Pharmaceutical Sciences 10, no. 4 (2019): 3694–703. http://dx.doi.org/10.26452/ijrps.v10i4.1756.

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The recent emergence of extensively drug-resistant tuberculosis has become a cause of concern for the management of tuberculosis globally. Shikimic acid pathway seems to be a potential and favorable target for the drug design of new anti-infective agents. This work aims to change the focus from traditional cell approaches to the target-based design of novel thiadiazolyl-azetidinone derivatives with Shikimate kinase as the drug target for anti-tubercular activity. Thiadiazole and azetidinone derivatives were methodically reprised to design a series of 3-chloro-4-(aryl)-1-(5-sulfanyl-1,3,4-thiadiazol-2-yl)azetidin-2-one derivatives (AZ1-AZ12). Molecular docking studies were performed on a crystal model of Mycobacterium tuberculosis Shikimate kinase (MtSK) using Vlife MDS 4.4 suite to evaluate their anti-tubercular potential. Further, drug-likeness properties and ADMET prediction were performed by molinspiration and admetSAR software to better describe the designed molecules as prospective candidates. 3-chloro-4-(4-nitrophenyl)-1-(5-sulfanyl-1,3,4-thiadiazol-2-yl)azetidin-2-one (AZ3), was found to be have better dock score when compared with the natural substrate, Shikimate. Docking studies confirmed that the molecules showed significant binding in the active site region of Shikimate kinase. Strong hydrogen bonding and hydrophobic interactions with amino acid residues and other parameters further explicate their effectiveness for inhibition of MtSK. Also, the physicochemical properties and drug scores for the designed compounds obtained by in silico studies were found to be satisfactory, signifying the overall potential of the designed molecules to be drug candidates. Thus these molecules could be explored as a lead for further anti-tubercular studies with Mycobacterium tuberculosis Shikimate kinase as the drug target.

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Moskvina, Viktoria, Olexander Turov, Tetyana Shokol, and Volodymyr Khilya. "Synthesis and NMR spectroscopy investigations of functionalized spiropyranochromenediones and their spirothiadiazole derivatives." Ukrainica Bioorganica Acta 16, no. 2 (2021): 18–22. http://dx.doi.org/10.15407/bioorganica2021.02.018.

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This investigation focuses on the synthesis of spiropyranoneoflavones and the modification of obtained compounds at the exocyclic oxygen atom. Kabbe cyclization of 6-acetyl-7‑hydroxy-8-methyl-4-phenyl-2H-chromene-2-one with cyclohexanone or cyclopentanone in the presence of pyrrolidine provided 10-methyl-4-phenyl-2H-spiro[cyclohexane(cyclopentane)-1’,8-pyrano[3,2-g]chromene]-2,6(7H)-diones. Their new functionalized derivatives with thiosemicarbazide residues were synthesized. Acetylation of obtained thiosemicarbazones with acetic anhydride proceeded via cyclization of thiosemicarbazide fragment into 1,3,4-thiadiazole ring to give corresponding N-[3'-acetyl-10-methyl-8-oxo-6-phenyl-3'H,8H-dispiro[cyclohexane-1,2’-pyrano[3,2-g]chromene-4,2'-[1,3,4]thiadiazol]-5'-yl]acetamide and N-[3'-acetyl-10-methyl-8-oxo-6-phenyl-3'H,8H-dispiro[cyclopentane-1,2’-pyrano[3,2-g]chromene-4,2'-[1,3,4]thiadiazol]-5'-yl]acetamide. The structure of the obtained compounds was confirmed by NMR spectroscopy

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Barlin, GB. "Heterocyclic Amplifiers of Phleomycin. VIII. Mono- Bis-(5'-substituted 1',3',4'-thiadiazol-2'-yl)pyridines and Mono(5'-substituted 1',3',4'-thiadiazol-2'-ylmethyl)pyridines." Australian Journal of Chemistry 38, no. 10 (1985): 1491. http://dx.doi.org/10.1071/ch9851491.

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A series of mono- and bis -(5′-substituted 1′,3′,4′-thiadiazol-2′- yl )pyridines with strongly basic side chains, e.g., 3,5-bis[5′(2′-N,N- dimethylaminoethylthio )-1′,3′,4′-thiadiazol-2′-yl]pyridine (1), and (5?-substituted 1′,3′,4′-thiadiazol-2′-ylmethyl)pyridines have been prepared for evaluation as amplifiers of phleomycin. Five of the six bis (5′-substituted 1′,3′,4′-thiadiazol-2′-yl)pyridines were themselves antibacterial under the test conditions, but compound (1) and the mono(5′-substituted 1′,3′,4′-thiadiazol-2′-yl)-pyridines and -methylpyridines displayed moderate two-to-three-star activity.

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Hashem, Aya B., Olfat A. Nief, and Abdulkader M. Noori. "Synthesis, Characterization, and Antimicrobial Evaluation of Thiadiazole Derivatives Derived from 2-Amino-5-Thio-1,3,4-Thiadiazole." Iraqi Journal of Industrial Research 11, no. 2 (2024): 87–96. http://dx.doi.org/10.53523/ijoirvol11i2id402.

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This manuscript introduces a series of novel Schiff base and heterocyc-licring compounds, focusing on derivatives of 1,3-oxazepine and thiazo-lidinone.The derivative (2-Hydroxy-N-(5-mercapto-[1,3,4] thiadiazol-2-yl)-2-phenyl-acetamide was created by reacting ethyl mandelate ester[M1] and 2-amino-5-thio-1,3,4-thiadiazole compound to produce new compound [M2] and after that, compound [M2] was reacted with hydrazine hydrate 99% in dry DMF solvent, yielding the compound (N-(5-Hydrazino-[1,3,4]thiadiazol-2-yl)-2-hydroxy-2-phenyl-acetamide [M3]. In contrast , the Schiff base compound [M4] were synthesized by reacting compound [M3] with aromatic heterocyclic aldehyde (furan-2-carbaldehyde) in the presence of glacial acetic acid as a catalyst, and then Schiff base [M4] was reacted with maleic anhydride in dry benzene as a solvent to produce (1,3-Oxazepine) derivative [M5]. Additionally, the thiazolidinone derivative [M6] was synthesized through the reaction of equimolar amounts of (N-[5-(N'-Furan-2-yl-methylene-hydrazino)-[1,3,4]thiadiazol-2-yl]-2-hydroxy-2-phenyl-acetamide [M4] with thioacetic acid compound in chloroform as a solvent. The structural formula of all derivatives was confirmed by FT-IR and (1HNMR, 13CNMR) spectroscopy. The synthesized derivatives [M1-M6] were screened for their evaluated for antibacterial activity against S. aureus, S. epidermidis, E. coli, Klebsiella sp., and the fungus Candida albicans. Dimethyl sulfoxide (DMSO) was used as the solvent. Also, the ampicillin compound was used as the standard drug for comparison.

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Rusul Mohammed Hasan Ali and Ayad Al-Hamashi. "Design, Synthesis, and Preliminary Antiproliferative Evaluation of 1,2,4-Thiadiazole Derivatives as Possible Histone Deacetylase Inhibitors." Iraqi Journal of Pharmaceutical Sciences 33, (4SI) (2025): 57–66. https://doi.org/10.31351/vol33iss(4si)pp57-66.

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Histone deacetylases (HDACs) are a class of proteins that responsible of the hydrolysis of N-acetyl lysine residues in histones as well as non-histone protein substrates. This phenomenon may provide an explanation for the involvement of these enzymes in a wide range of clinical situations, encompassing cancer, metabolic, cardiovascular problems, and neurological diseases. Most of HDAC inhibitors are often used in clinical settings consist of a hydroxamate group (ZBG) that binds to zinc ion inside the active site. The poor selectivity and pharmacokinetic characteristics of numerous medicines belonging to the hydroxamates group have prompted the exploration of non-hydroximic ZBG HDAC inhibitors with a potential selectivity and potency profile. Therefore, the objective of this work is to design new HDAC inhibitors incorporating thiadiazole moiety as a ZBG. This study involved the design and virtual analysis of a series of thiadiazole derivatives using Maestro software. Compounds with good docking score which include compound 6a [4- (benzyloxy)-N-(1,2,4-thiadiazol-5-yl)benzamide] with docking score -8.953 kcal/mol and compound 6b [4-(naphthalen-1-ylmethoxy)-N-(1,2,4-thiadiazol-5- yl)benzamide] with docking score -9.290 kcal/mol and compound 6c[ 4-((4-methoxybenzyl)oxy)benzoic acid] with docking score -8.57 kcal/mol while the FDA approved vorinostat has a docking score -5.613 kcal/mol against HDAC 2 (4LXZ). Compound 6a, 6b and 6c were subjected to the organic synthesis applying traditional chemical reactions. The synthesis was commenced with the ether formation using Williamson reaction by reacting benzylic bromide derivatives with methyl 4-hydroxybenzoate, then the intermediates underwent ester hydrolysis to produce 4-(benzyloxy)benzoic acid derivatives and then reacted with 1,2,4-thiadiazol-5- amine by forming amide using 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) as coupling reagent. The intermediates and final products were characterized by FT-IR and NMR spectroscopy. The cytotoxic effect was assessed using the MTT cell viability assay indicate that IC50 of 6b is 0.66 μM while the IC50 of vorinostat is 1.48 μM.

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Gudim, Nikita S., Ekaterina A. Knyazeva, and Oleg A. Rakitin. "7,7’-(4,4-Bis(2-ethylhexyl)-4H-cyclopenta[2,1-b:3,4-b’]dithiophene-2,6-diyl)bis(4-bromobenzo[c][1,2,5]thiadiazole)." Molbank 2022, no. 1 (2021): M1310. http://dx.doi.org/10.3390/m1310.

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2,6-Bis(benzo[c][1,2,5]thiadiazol-4-yl)-4H-cyclopenta[2,1-b:3,4-b’]dithiophenes are of interest for the synthesis of molecules which can be employed in optoelectronic devices. In this communication, 7,7’-(4,4-bis(2-ethylhexyl)-4H-cyclopenta[2,1-b:3,4-b’]dithiophene-2,6-diyl)bis(4-bromobenzo[c][1,2,5]thiadiazole) was obtained by direct C–H cross-coupling of 4,7-dibromobenzo[c][1,2,5]thiadiazole with 4,4-bis(2-ethylhexyl)-4H-cyclopenta[2,1-b:3,4-b’]dithiophene in the presence of palladium(II)acetate and potassium pivalate. The structure of newly synthesized compound was established by means of elemental analysis, high-resolution mass spectrometry, 1H, 13C NMR, IR and UV spectroscopy.

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Igor, Sych, Bevz Natalia, Sych Irina, Rakhimova Maryna, Yaremenko Vitaliy, and Perekhoda Lina. "Development of quality control methods of promising anticonvulsant." ScienceRise: Pharmaceutical Science, no. 6(16) (December 28, 2018): 13–21. https://doi.org/10.15587/2519-4852.2018.152837.

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In the previous studies, NUPh scientists proved that the search of potential anticonvulsants among derivatives of 1,3,4-thiadiazole is very perspective [1-3]. At the medicinal chemistry department of NUPh N-(5-ethyl-[1,3,4]-thiadiazole-2-yl)-2-nitrobenzamide was synthesized. This substance demonstrated high anticonvulsive activity on pentylentetrazole model of seizure compared to classic drug «Depakin». The substance is patented and proposed for further preclinical studies. One of the most important stages in the introduction of a new medicinal product or substance into medical practice is the development of quality control techniques. The aim. The aim of this work was to develop methods of identification, determination of impurities and quantitative determination of N- (5-ethyl- [1,3,4] -thiadiazole-2-yl)-2-nitrobenzamide for further application in standardization of the substance. Methods. Chromatographically pure sample of N- (5-ethyl- [1,3,4] -thiadiazole-2-yl) -2-nitrobenzamide, methods of IR, UV and 1H NMR spectroscopy. Results. The physical-chemical properties and spectral characteristics of N-(5-ethyl-[1,3,4]-thiadiazole-2-yl)-2-nitrobenzamide were studied, and chemical identification methods were proposed. The optimal conditions for the determination of the impurities by the method of thin-layer chromatography using the method of internal normalization are selected. The assay for N- (5-ethyl- [1,3,4] -thiadiazol-2-yl) -2-nitrobenzamide was carried out by absorption spectrophotometry in the alcohol solution at the wavelength of 282 nm with the absorption index 631. For application of methods such validation characteristics as robustness, linearity, correctness, stability of analytical solutions, precision, convergence, reproducibility, calculation of uncertainty of samples preparation were studied. Conclusions. The methods of identification of N- (5-ethyl- [1,3,4] -thiadiazol-2-yl) -2-nitrobenzamide with the use of chemical reactions and spectral methods of analysis - IR and UV and 1H NMR spectroscopy have been developed. To determine the concomitant impurities in the substance, the TLC method is recommended. Specific and nonspecific impurities were determined. The method of quantitative determination of substance by absorption spectrophotometry method in the ultraviolet region by the method of specific absorption index have been developed

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Merugu, Shivanand, Vijaya Kumar Ponnamaneni, Ravi Varala, et al. "Metal-free Catalyzed One-Pot Multicomponent Synthesis of (E)-3-(2-((5-(Benzylideneamino)-1,3,4-thiadiazol-2-yl)thio) Acetyl)-2H-chromen-2-one Derivatives and Their Biological Evaluation." Journal of Chemistry 2020 (April 10, 2020): 1–7. http://dx.doi.org/10.1155/2020/4869279.

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A series of (E)-3-(2-((5-(benzylideneamino)-1,3,4-thiadiazol-2-yl)thio) acetyl)-2H-chromen-2-one and its derivatives (4a-h) have been obtained using a one-pot multicomponent reaction with good yields. The compounds have been synthesized from 3-(2-bromoacetyl)chromen-2-ones (1), 5-amino-1,3,4-thiadiazole-2-thiol (2), and substituted benzaldehydes (3) in anhydrous ethanol and conc. H2SO4. Subsequently, all the synthesized compounds have been screened for their antimicrobial activity and characterized by analytical and spectral data.

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Kurup, Rishi R., Rakhi Mishra, Rupa Mazumder, and Avijit Mazumder. "Synthesis and evaluation of anti-convulsant activity of some new pyridylthiadiazole derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 541. https://doi.org/10.59467/ijhc.2025.35.541.

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The synthesis of some new 5-(pyridin-3-ylamino)-1,3,4-thiadiazole-2-carboxamides, 5-(pyridin-3-ylamino)- 1,3,4-thiadiazole-2-carboxylates and (1H-benzo[d]imidazol-6-yl)(5-(pyridin-3-ylamino)-1,3,4-thiadiazol-2-yl) methanone was accomplished by the reaction of 5-(pyridin-3-ylamino)-1,3,4-thiadiazole-2-carbonyl chloride with a substituted alcohols, amines and benzimidazole through amide and ester link formation at the thiadiazole ring. Molecular docking parameters assessed the potential of derivatives through CB2-dock software, and the docking score of the derivatives varied from the range of -6.6_-9.2 Kcal/Mole against the targeted GABA(A)R-beta3 homopentamer receptor (PDB ID: 4COF). An investigation of the anti-convulsant activity on Swiss albino mice was performed through maximal electroshock and scPTZ tests, using phenytoin as a standard drug. The derivatives 8c and 9 showed maximum potency among all the prepared derivatives compared to the phenytoin drug.. KEYWORDS :Anti-convulsant, Molecular docking, Maximal electroshock, Pyridylthiadiazole.

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Almasirad, Ali, Loghman Firoozpour, Maliheh Nejati, et al. "Design, synthesis, and biological evaluation of new series of 2-amido-1,3,4-thiadiazole derivatives as cytotoxic agents." Zeitschrift für Naturforschung B 71, no. 3 (2016): 205–10. http://dx.doi.org/10.1515/znb-2015-0138.

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AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.

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S., D. Srivastava, and Guru Niharika. "Synthesis and antimicrobial activities of some new pyrazolothiadiazoles and their azetidinones." Journal of Indian Chemical Society Vol. 77, Aug 2000 (2000): 400–401. https://doi.org/10.5281/zenodo.5869215.

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Department of Chemistry, Dr. H. S. Gour University, Sagar-470 003, India Manuscript received 4 November 1999, revised 27 March 2000, accepted 17 April 2000 Several 2-arylideneamino-5-(N1-pyrazolomethyl)-1,3,4-thiadiazoles (4) and 1-[5' -(N1-pyrazolomethyl)-1' ,3',4' -thiadiazol-2'-yl]-4-substituted-3-chloro-2-azetidinones (5) have been synthesised and tested for their antibacterial and antifungal activities.

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