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Journal articles on the topic '4-triazole derivatives'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

Karpun, Yevhen, and Nataliia Polishchuk. "Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol." ScienceRise: Pharmaceutical Science, no. 3(31) (June 30, 2021): 64–69. http://dx.doi.org/10.15587/2519-4852.2021.235976.

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The aim of the work. 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)t

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2

Yevhen, Karpun, and Polishchuk Nataliia. "Synthesis and antimicrobial activity of s-substituted derivatives of 1,2,4-triazol-3-thiol." ScienceRise: Pharmaceutical Science, no. 3(31) (June 30, 2021): 64–69. https://doi.org/10.15587/2519-4852.2021.235976.

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<strong>The aim of the work.</strong> 1,2,4-triazole derivatives possess a wide range of pharmacological activity, so they are used for the development of drugs and active pharmaceutical ingredients. Due to the reactivity of 1,2,4-triazoles there are many options for their further structural modification on different reaction centers. Therefore, the aim of the work was to obtain new S-substituted derivatives of 1,2,4-triazole-3-thiols, study physicochemical parameters of the substances synthesized, evaluate the antimicrobial activity of new S-derivatives of the 4-R1-5-((3-(pyridin-4-yl)-1

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3

Syrota, Natalia O., Sergiy V. Kemskiy, Lesya M. Saliyeva, and Mykhailo V. Vovk. "1,2,3-Triazole-4(5)-amines – Convenient Synthetic Blocks for the Construction of Triazolo-Annulated Heterocycles." Journal of Organic and Pharmaceutical Chemistry 20, no. 2 (2022): 27–51. http://dx.doi.org/10.24959/ophcj.22.258512.

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Aim. To analyze and summarize the synthetic potential of 1,2,3-triazole-4(5)-amines as efficient building blocks in the synthesis of triazolo-annulated pyridine, azine and azepine systems.Results and discussion. Original literature sources revealing the synthetic potential of 4(5)-amino functionalized 1,2,3-triazoles as convenient and available building blocks for the preparation of triazolo-annulated pyridines, azines and azepines were analyzed and systematized. Condensation of 1,2,3-triazole-4(5)-amines with methylene active compounds was shown to be a powerful tool for the synthesis of vers

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4

GAMAL, A. AHMED. "Studies on 3-Amino-I ,2,4-triazole." Journal of Indian Chemical Society Vol. 74, Aug 1997 (1997): 624–25. https://doi.org/10.5281/zenodo.5891468.

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Department of Chemistry , Faculty of Science, Zagazig University, Zagazig, Egypt <em>Manuscript received 16 October 1995, revised 18 June 1996, accepted 24 July 1996</em> 1,2,4-Triazolo[2,3-a]-1,3,5-triazine-4-aryl-4-thiones (3a,b) and 5-(aroylamino)-1,2,4-triazoles (5a,b) have been synthesised by the reaction of 3-amino-1,2,4-triazole (1) with aroyl isothiocyanates. Also, 1 when reacted with cinnamonitrile derivatives yields the trlazolopyrimldine derivatives (6, 7a,b and 8). Treatment of 8 with carbon disulphide and formaide gives 9 and 10 respectively. Some of the compounds possess antimicr

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5

Murthy Appala, Venkata Ramana, Kanaka Durga Bhavani Anagani, and Aparna Pasula. "Synthesis of New Piperidine based N(2)-Alkylated 1,2,3-Triazole Hybrids in Basic Medium." Asian Journal of Chemistry 35, no. 1 (2022): 212–16. http://dx.doi.org/10.14233/ajchem.2023.26906.

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The nucleophilic reaction of 1H-triazole derivatives with piperidines under basic conditions is the essential step in the synthesis of a new series of dibenzyl N(2)-C-linked triazolyl piperidines. The triazole derivative was synthesized via the CuAAc reaction of 1-phenylprop-2-yn-1-ol (1a-b) with azidomethyl pivalate. Compound 3a-b underwent dehydroxylation and deprotection reactions using TFA, triethyl silane and 1 M NaOH respectively, yielding monobenzyl 1H-1,2,3-triazole (4a-b). The N(2)-piperidinyltriazoles (6a-j) were synthesized in significant amounts by nucleophilically reacting 1H-tria

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6

Gotsulya, A. S., A. I. Panasenko, E. G. Knysh, and A. O. Pryimenko. "UV-spectrophotometric study of the 7-((3-thio-4-R-1,2,4-triazole-3-yl)methyl)-theophyllines." Farmatsevtychnyi zhurnal, no. 4 (September 4, 2018): 65–70. http://dx.doi.org/10.32352/0367-3057.4.15.03.

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Chemistry of the 1,2,4-triazole derivatives recently attracts the attention of many scientists, mainly due to the presence of the number of the valuable pharmacological properties. In modern medical practice, there are many examples of successful heterocyclic systems derivatives usage. First of all, it is a group of drugs with antifungal activity (fluconazole, itraconazole, voriconazole, pozakonazol), antidepressant activity (alprazolam, triazolam), anticancer activity (anastrozole, letrozole). But despite the great practical importance of works in this area, the structure of 1,2,4-triazoles-3

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7

Frolova, Yu S., A. H. Kaplaushenko, T. V. Ihnatova, and T. M. Kaplaushenko. "Synthesis methods of 1,2,4-triazole-3-thiones: review." Current issues in pharmacy and medicine: science and practice 17, no. 2 (2024): 187–96. http://dx.doi.org/10.14739/2409-2932.2024.2.302616.

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1,2,4-Triazole-containing compounds are unique heterocyclic compounds present in an array of pharmaceuticals and biologically important compounds used in drug-discovery studies against cancer cells, microbes, and various types of diseases in the human body. The aim of the study was to analyze in detail and combine the available literature materials to study the reactions associated with the formation of different classes of derivatives of 1,2,4-triazole-3-thione and to study their physical-chemical properties. Various innovative methods have been proposed and explored for synthesizing differen

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8

Shakeel Ahmed, Shiza Murad, Iqra Munir, et al. "Spectroscopic Investigation and Synthesis of N-Ethyl-5-Tolyloxymethyl Triazole Derivatives." Indus Journal of Bioscience Research 3, no. 5 (2025): 288–96. https://doi.org/10.70749/ijbr.v3i5.1234.

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High-nitrogen heterocycles' synthesis has attracted much interest because of their wide applicability in many different sectors. As a significant class of organic compounds, triazoles and their fused derivatives have emerged among these. A new triazole derivative, 4-ethyl-3-ethylthio-5-(p-tolyloxymethyl)-4H-1, 2, 4-triazole, is the subject of this work on synthesis and spectrum characterization. Ethyl 2-p-tolyloxy acetate is synthesized by reacting 3, 4-dimethoxyphenylacetic acid with ethanol under concentrated H2SO4, starting the process. The ester product is subsequently transformed into 2-p

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9

Hryhorka, H. V., М. М. Fizer, О. І. Fizer, A. O. Kryvoviaz, and M. V. Slivka. "SYNTHESIS AND CHEMICAL PROPERTIES OF 2-HEPTADECYL-[1,3]THIAZOLO[3,2-b][1,2,4]TRIAZOL-7-IUM CATION." Scientific Bulletin of the Uzhhorod University. Series «Chemistry» 48, no. 2 (2023): 67–72. http://dx.doi.org/10.24144/2414-0260.2022.2.67-72.

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Functional and condensed derivatives of 1,2,4-triazoles are mostly used as biologically active compounds, and modern studies increasingly report their successful use as surfactants, stabilizers for the formation of nanoparticles, components of hybrid perovskites, which are promising materials for opto-electronics. Synthesis of new [1,3]thiazolo[3,2-b][1,2,4]triazol-7-ium salts containing a long-chain heptadecyl substituent was proposed within our research. The production of the starting compounds (2-heptadecyl-4-methyl-1,2,4-triazole-3-thione and methallyl thioether of 2-heptadecyl-3-mer

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10

Md, Akram* Abdul Sayeed Mohd Waseem Akram MD Ather Ali Soherwardi. "STUDIES ON THE SYNTHESIS OF SOME NEW 1,2,4- TRIAZOLES DERIVATIVES AND EVALUATION FOR THEIR ANTI-FUNGAL ACTIVITY PROFILES." Indo American Journal of Pharmaceutical Sciences 04, no. 08 (2017): 2234–48. https://doi.org/10.5281/zenodo.839545.

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The synthesis of new heterocyclic compounds has always drawn the attention of medicinal chemist over the years mainly because they possess diverse biological properties. The literature survey on 1,2,4-triazoles revealed that they are endowed with wide variety of biological activities .During the present investigation a series of new 1,2,4-triazole derivatives N-(3-(2-(3- hydrazinyl-3-oxoalkanoyl)hydrazinyl)-5-(phenoxymethyl)-4H-1,2,4-triazol-4-yl)isonicotinamide(6a- 6e)were synthesized by reacting withN-(5-mercapto-3-(phenoxymethyl)-4H-1,2,4-triazol-4- yl)isonicotinamide (5) and aliphatic dica

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11

Maj, Anna, Agnieszka Kudelko, and Marcin Świątkowski. "Novel Conjugated s-Tetrazine Derivatives Bearing a 4H-1,2,4-Triazole Scaffold: Synthesis and Luminescent Properties." Molecules 27, no. 2 (2022): 459. http://dx.doi.org/10.3390/molecules27020459.

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A series of new symmetrical s-tetrazine derivatives, coupled via a 1,4-phenylene linkage with a 4H-1,2,4-triazole ring, were obtained. The combination of these two rings in an extensively coupled system has significant potential applications, mainly in optoelectronics. The methodology used turned out to be useful regardless of the type of five-membered ring or the nature of the individual substituents. All the products were identified by spectroscopic methods, and the target compounds were tested for luminescent properties. This study showed that all the synthesized highly-conjugated triazoles

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12

Bilai, I. M., V. I. Dariy, A. V. Khilkovets, and A. I. Bilai. "Current research trends of 1,2,4-triazole derivatives biological activity (literature review)." Current issues in pharmacy and medicine: science and practice 18, no. 2 (2025): 197–205. https://doi.org/10.14739/2409-2932.2025.2.322344.

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The relevance of searching for new active compounds among 1,2,4-triazole derivatives is determined by their potential effectiveness in treating various diseases such as cancer, inflammation, microbial infections, and antioxidant disorders. Studies show that these compounds can inhibit the proliferation of cancer cells, exhibit anti-inflammatory properties, demonstrate activity against pathogenic microorganisms, and neutralize free radicals, which is important for preventing oxidative stress. Therefore, the study of 1,2,4-triazole derivatives may lead to the development of new effective drugs,

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13

Choudhary, Sunil Kumar, Priya Gothwal, Nidhi Sogani, Ajay Saini, and Suman Swami. "Rational Design, Synthesis, Characterization, and Anti-bacterial activity of Urea Derivatives Bearing 1,2,4-triazoles as Molecular Hybrid Scaffolds." Oriental Journal Of Chemistry 39, no. 1 (2023): 129–35. http://dx.doi.org/10.13005/ojc/390115.

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A new set of molecular hybrids, urea derivatives carrying 1,2,4-triazole as molecular hybrid scaffolds, were developed, synthesised, characterised, and assessed for potential anti-bacterial action. Triazole scaffolds are key moieties in many pharmacological compounds, and their inclusion with urea moiety makes them more valuable for biological purposes. As a result, urea derivatives containing 1H-1,2,4-triazole and 3-(methylthio)-1H-1,2,4-triazole moieties were produced by reacting carbamates of 4-amino-1,2,4-triazoles and 3-(methylthio)-4-amino-1,2,4-triazole with amines in DMF using trimethy

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14

Janam Singh, Ram, and Dharmendra Kumar Singh. "Syntheses of Some 3,5-Diaryl-4H-1,2,4-triazole Derivatives and their Antifungal Activity." E-Journal of Chemistry 6, s1 (2009): S219—S224. http://dx.doi.org/10.1155/2009/925964.

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Syntheses of a series of 3, 5-diaryl-4H-1, 2, 4-triazole derivatives are described. In this present work, 4-amino-3-phenyl-5-p-tolyl-4H-1,2,4-triazole(1) was converted toN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine(2) and 3-Phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) in good yields by treatment with aldehydes OHC-C6H4-CHO and Ar-CHO respectively. The compoundsN,N’-bis[3-phenyl-5-p-tolyl-4H-1,2,4-triazolyl]-1,4-xylenediimine (2) and 3-phenyl-5-p-tolyl-4-[4-methyl benzylidenamino]-4H-1,2,4-triazole (3) were reduced with NaBH4to afford the correspondin

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15

Dobosz, Maria, Monika Pitucha, Izabela Dybala, and Anna E. Kozioł. "Cyclization of Semicarbazide Derivatives of 3-Methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetic Acid." Collection of Czechoslovak Chemical Communications 68, no. 4 (2003): 792–800. http://dx.doi.org/10.1135/cccc20030792.

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By the reaction of hydrazide of 3-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetic acid (1) with isocyanates, 3-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazole-4-acetosemicarbazide derivatives 2 were obtained. Cyclization of these compounds in the presence of 2% NaOH led to the formation of 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives 3, which was confirmed by X-ray analysis of 3b.

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16

Rathmann, Stephanie M., Nancy Janzen, and John F. Valliant. "Synthesis, radiolabelling, and biodistribution studies of triazole derivatives for targeting melanoma." Canadian Journal of Chemistry 94, no. 9 (2016): 773–80. http://dx.doi.org/10.1139/cjc-2016-0239.

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Molecular probes that target specific markers expressed in solid tumours are in demand for cancer imaging and radionuclide therapy applications. The synthesis, characterization, and in vivo evaluation of radioiodinated triazoles designed as probes to target melanoma are described here. Compounds were prepared using a thermal click reaction between ethynylstannane and methyl 2-azidoacetate, resulting in preferential formation of the corresponding 1,4-tin triazole. The primary amine of various targeting vectors was then coupled to the resulting tin triazole methyl ester. These precursors were la

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17

Karpun, E. O., and V. V. Parchenko. "Synthesis, physicochemical properties and antigypoxic activity of some S-derivatives of 4-alkyl-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)methyl)-4H-1,2,4-triazole-3-thiol." Farmatsevtychnyi zhurnal, no. 6 (December 9, 2020): 56–64. http://dx.doi.org/10.32352/0367-3057.6.20.06.

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Hypoxia is a discrepancy between the required energy of the cell in the mitochondrial oxidative phosphorylation system. The immediate cause of the deficiency is a decrease in the oxygen concentration in the mitochondria. Today there is a huge demand for the development of new anti-hypoxic drugs. t is known that 1,2,4-triazole compounds can have antimicrobial, anti-inflammatory, anti-hypoxic effects. Modification of the 1,2,4-triazole nucleus is a productive way to create original active molecules with a non-planar structure, for their binding to bio-target substrates. Derivatives of bis-1,2,4-

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18

Onisko, Mikhailo. "ARYLTELLUROCHLORINATION OF 5-ARYL(HETERYL)SUBSTITUTED N-ALLYL-1,2,4-TRIAZOLE-3-THIONE DERIVATIVES." Ukrainian Chemistry Journal 89, no. 8 (2023): 109–16. http://dx.doi.org/10.33609/2708-129x.89.08.2023.109-116.

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Condensed heterocycles based on 1,2,4-triazole have a wide range of biological activity. The introduction of a pharmacophore fragment of an aryl tertiary residue into their composition can significantly increase the bioactivity of the obtained compounds. Therefore, the synthesis of condensed derivatives of symmetrical 1,2,4-triazole with aryltellurium fragment is an urgent task. One of the most convenient and effective methods for introducing an aryltellurium fragment into such systems is the method of electrophilic intramolecular cyclisation of alkenyl derivatives of azaheterocycles. The aim

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19

Schepetkin, Igor A., Zhangeldy S. Nurmaganbetov, Serik D. Fazylov, et al. "Inhibition of Acetylcholinesterase by Novel Lupinine Derivatives." Molecules 28, no. 8 (2023): 3357. http://dx.doi.org/10.3390/molecules28083357.

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Alzheimer’s disease (AD) is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment due in part to a severe loss of cholinergic neurons in specific brain areas. AD is the most common type of dementia in the aging population. Although several acetylcholinesterase (AChE) inhibitors are currently available, their performance sometimes yields unexpected results. Thus, research is ongoing to find potentially therapeutic AChE inhibitory agents, both from natural and synthetic sources. Here, we synthesized 13 new lupinine triazole derivatives and evaluated them,

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20

Sabzi, Noor Ali, and May Mohammed Jawad. "Synthesis, Characterization, and Preliminary Evaluation of Antimicrobial activity of Imines derived from Vanillic Acid Conjugated to Heterocyclic." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 32, Suppl. (2023): 8–15. http://dx.doi.org/10.31351/vol32isssuppl.pp8-15.

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The purpose of this research is to prepare new vanillic acid derivatives with 1,2,4-triazole-3-thiol heterocyclic ring and evaluate their antimicrobial activity in a preliminary assessment. A multistep synthesis was established for the preparation of new vanillic acid-triazole conjugates. The intermediate of 4-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)-2-methoxyphenol (4) reacts with different heterocyclic aldehydes (thiophene-2-carboxaldehyde, pyrrole-2-carboxaldehyde, thiophene-3-carboxaldehyde, and furfural ) in ethanol containing few drops of acetic acid yielded the corresponding 4-(4-(sub

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21

Gribanov, Pavel S., Anna N. Philippova, Alexander F. Smol’yakov, et al. "Synthesis of Functionalized 1H-Imidazoles via Denitrogenative Transformation of 5-Amino-1,2,3-Triazoles." Molecules 30, no. 7 (2025): 1401. https://doi.org/10.3390/molecules30071401.

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An efficient access to novel 2-substituted 1H-imidazole derivatives was developed based on acid-mediated denitrogenative transformation of 5-amino-1,2,3-triazole derivatives available through dipolar azide−nitrile cycloaddition (DCR). The proposed approach includes intramolecular cyclization of 5-amino-4-aryl-1-(2,2-diethoxyethyl) 1,2,3-triazoles followed by triazole ring opening and insertion of in situ formed carbene intermediate into the O-H bond of different alcohols under acidic conditions.

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22

Safonov, A. A. "Synthesis, physico-chemical properties of derivatives 3-(alkylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-4-amine." Farmatsevtychnyi zhurnal, no. 3-4 (August 14, 2018): 50–54. http://dx.doi.org/10.32352/0367-3057.3-4.16.03.

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Recently, the search for new compounds with high biological activity, which can be the basis for potential drugs, becomes topical for world scientists. A heterocyclic compound cause particular interest in this area as highly pharmacologically active compounds. Scientists extends interest due to the low toxicity and high reactivity 1,2,4-triazole of the system. It is proved that the combination of triazole nucleus with other heterocyclic systems, especially in the fifth position, causes increased biological effect, and, sometimes, the appearance of new pharmacological activities. The aim

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23

Jalihal, Prabhu C., Vaibhav Rajoriya, and Varsha Kashaw. "DESIGN, SYNTHESIS, AND EVALUATION OF NEW DERIVATIVE OF 1,2,4-TRIAZOLES FOR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTIVITY." International Journal of Current Pharmaceutical Research 10, no. 4 (2018): 29. http://dx.doi.org/10.22159/ijcpr.2018v10i4.28455.

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Objective: The object of the study is to design, synthesize and biological evaluation of isoniazid derived 1,2,4-triazoles compounds.Methods: Isoniazid based 1,2,4-triazoles derivatives have been synthesized by reaction of Isoniazid with carbon disulfide in basic medium (KOH) to form Potassium dithiocarbazinate salt and reaction with hydrazine hydrate converted into 4-amino-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol. These compounds were reacted with seven different benzaldehyde to form 4-[(substituted phenyl)-methylene]-amino-5-(pyridine-4-yl)-4H-1,2,4-triazol-3-thiol (4). The final compounds

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24

Neelgundmath, Mahabaleshwaraiah, and Oblennavar Kotresh. "Synthesis, Evaluation and Characterization of Some 1,3,4-Triazole-2-one Derivatives as Antimicrobial Agents." E-Journal of Chemistry 9, no. 4 (2012): 2407–14. http://dx.doi.org/10.1155/2012/672125.

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A series of novel compounds like 3[(phenyl substituted)-5-methyl-1(Benzosulphonylamine)]-1,3,4-triazole-2-ones II(a-f) were synthesized by treating 4-amino-1-phenyl-3-methyl-5-oxo-1,2,4-triazoles with benzene sulphonyl chloride using pyridine as solvent. Similarly by using 4-amino-1-aryl-3-methyl-5-oxo-1,2,4-triazoles and acetic anhydride as starting material 3[(phenyl substituted)-5-methyl-1(acetylamino)]-1,3,4-triazole-2-ones III(a-f) were synthesized and also 3[(phenyl substituted)-5-methyl-1(chloroacetyl)]-1,3,4-triazole-2-ones I(a-f) were synthesized by treating 4-amino-1-aryl-3-methyl-5-

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25

Xiao, Pan-Lei, Xiu-Ying Song, Xin-Ting Xiong, Da-Yong Peng, and Xu-Liang Nie. "Synthesis, Crystal Structure, Spectral Characterization and Antifungal Activity of Novel Phenolic Acid Triazole Derivatives." Molecules 28, no. 19 (2023): 6970. http://dx.doi.org/10.3390/molecules28196970.

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At present, phenolic acid derivatives and triazole derivatives have a good antifungal effect, which has attracted widespread attention. A series of novel phenolic acid triazole derivatives were synthesized, and their structures were characterized by IR, MS, NMR, and X-ray crystal diffraction. Compound methyl 4-(2-bromoethoxy)benzoate, methyl 4-(2-(1H-1,2,4-triazol-1-yl) ethoxy)benzoate, 4-(2-(1H-1,2,4-triazol-1-yl)ethoxy)benzoic acid and 4-(2-(1H-1,2,4-triazol-1-yl) ethoxy)-3-methoxybenzoic acid crystallize in the monoclinic system with space group P21/n, the monoclinic system with space group

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Reeta, Tripathi, Mishra Diwa, and Singh Arun. "Preparation and Antimicrobial Studies of Oxadiazine Containing Heterocyclic Compounds." International Journal of Trend in Scientific Research and Development 3, no. 5 (2019): 412–14. https://doi.org/10.5281/zenodo.3589858.

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The triazole derivative say 2 3 methylthio 5 phenyl 4H 1,2,4 triazol 4 yl acetohydrazide 1 was prepared. Various Schiff bases 3a e of 1 were prepared by reacting with various benzaldehyde derivatives 2a e . All the 3a e compounds condensed with benzoyl isothiocyanate 4 to afford N 2 aryl 6 phenyl 4 thioxo 2H 1,3,5 oxadiazin 3 4H yl 2 3 methylthio 5 phenyl 4H 1,2,4 triazol 4 yl acetamide derivatives 5a e . All the synthesized compounds characterized spectroscopically and tested for antimicrobial activity. Reeta Tripathi | Diwa Mishra | Arun Singh "Preparation and Antimicrobial Studies of O

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Elhady, A. N. El-Sharabasy A. S. Kassab S. R. R. Soliman A. M. F. &. Ali A. A. E. "New anticorrosion and flame retardant coating compositions based on 4-amino triazole derivatives , their Schiffs' bases and epoxy varnish." International Journal of Applied Research 6, no. 1 (2020): 60–72. https://doi.org/10.5281/zenodo.4013369.

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In this study, some recently amino triazole derivatives mainly 4-amino-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione(I),4-((furan-2-yl-methylene)amino)-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione(II), 4-((4-nitrobenzyl- idene)amino)-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (III),4-((4-(dimethylamino)benzylidene)amino)-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (IV), 5-phenyl-4-((3-phenyl-4-((3-phenylallylidene) amino)-2,4-dihydro-3H-1,2,4-triazole-3-thione(V),4-(((3-phenyl-5-thioxo-1,5-dihydro-4H-1,2,4-triazole-4yl)imino)methyl)benzal-  dehyde(VI),and3-(((3-phenyl-5-thio

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Sabzi, Noor Ali Hussein, and May Mohammed Jawad Al-Mudhafar. "Synthesis, characterization, and antimicrobial evaluation of new Schiff bases derived from vanillic acid conjugated to heterocyclic 4H-1,2,4-triazole-3-thiol." Pharmacia 70, no. 3 (2023): 657–63. http://dx.doi.org/10.3897/pharmacia.70.e104579.

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A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (4). Finally, several aromatized aldehydes reacted with compound (4) to produce Schiff bases derivatives (5–11). The purpose of this research is to prepare new vanillic acid derivatives with 1, 2, 4-triazole-3-thiol heterocyclic ring structures and to evaluate their antimicrobial activity in a preliminary assessment. Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance spectroscopy (1H-NMR) were used to verify the structures of the newly synthesized compounds

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Kalchenko, V. V., and R. O. Shcherbyna. "Computer prediction of toxicity of new S-alkyl derivatives of 1,2,4-triazole." Current issues in pharmacy and medicine: science and practice 17, no. 3 (2024): 253–56. http://dx.doi.org/10.14739/2409-2932.2024.3.312927.

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1,2,4-Triazole derivatives are of researchers’ significant interest due to their diverse biological properties, such as antimicrobial, anti-inflammatory, anticancer, and antioxidant activities. The integration of a 2-bromo-4-fluorophenyl fragment into the triazole structure can significantly enhance these activities. However, the evaluation of the toxicity of such compounds remains a critically important aspect for their practical application. To reduce the time and cost of experimental studies, QSAR (Quantitative Structure-Activity Relationship) methods are actively used, allowing the predict

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30

Maliszewska-Guz, Alicja, Monika Wujec, Monika Pitucha, et al. "Cyclization of 1-{[(4-Methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetyl}thiosemicarbazides to 1,2,4-Triazole and 1,3,4-Thiadiazole Derivatives and Their Pharmacological Properties." Collection of Czechoslovak Chemical Communications 70, no. 1 (2005): 51–62. http://dx.doi.org/10.1135/cccc20050051.

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By the reaction of 4-methyl-4H-1,2,4-triazole-3-thiol with ethyl bromoacetate, ethyl [(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetate (1) was obtained. This compound was converted to [(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]acetohydrazide (2). In the reaction of 2 with isothiocyanates, new thiosemicarbazides 3a-3g were obtained. The cyclization of 3a-3g in 2% aqueous solution of sodium hydroxide led to the formation of 4H-1,2,4-triazole-3(2H)-thione derivatives 4a-4g, whereas the cyclization in acid media led to the formation of 2-amino-1,3,4-thiadiazole derivatives 5a-5g. Molecular structur

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31

Kaplaushenko, Т. М., О. І. Panasenko та Y. G. Samelyuk. "Synthesis and establishment of physico-chemical constants 2-(5-( chinoline -2-il, 2-hydroxyquinoline-4-іл)-4-R1-1,2,4-triazole-3-ілтіо) acetate acids and their esther". Farmatsevtychnyi zhurnal, № 2 (14 серпня 2018): 53–59. http://dx.doi.org/10.32352/0367-3057.2.16.04.

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The large interest in the plan of search biologically of active agents is caused by the heterocyclic system of 1,2,4-triazole, due to high biological activity, and by the low indexes of toxicness, that inherent it to the structural analogues. Today in medical practice the derivatives of 1,2,4-triazole are used as high-efficiency antioxidants, cytostatic antimycotic agent , antidepressants and others. Literary information testify that among connections, representatives derivative of 3-tio-1,2,4-triazole range condensed with heteryl carboxylic acid, and their derivatives, find matters with

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32

Nurmaganbetov, Zhangeldy S., Oralgazy A. Nurkenov, Andrei I. Khlebnikov, et al. "Antiviral Activity of (1S,9aR)-1-[(1,2,3-Triazol-1-yl)methyl]octahydro-1H-quinolizines from the Alkaloid Lupinine." Molecules 29, no. 23 (2024): 5742. https://doi.org/10.3390/molecules29235742.

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Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)). The ability of (1S,9aR)-1-[(1,2,3-triazol-1-yl)-methyl]octahydro-1H-quinolizines with aryl-, 4-((4-formylphenoxy)methyl)- or 4-((3-tert-butyl-5-ethyl-2-hydroxy-

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33

Pandey, Vinod Kumar, Zehra Tusi, Sumerah Tusi, and Madhawanand Joshi. "Synthesis and Biological Evaluation of Some Novel 5-[(3-Aralkyl Amido/Imidoalkyl) Phenyl]-1,2,4-Triazolo[3,4-b]-1,3,4-Thiadiazines as Antiviral Agents." ISRN Organic Chemistry 2012 (September 11, 2012): 1–7. http://dx.doi.org/10.5402/2012/760517.

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A series of novel 4-amino-5-mercapto-3-[(3-aralkyl amido/imidoalkyl) phenyl]-1,2,4-triazoles (5a-d) were obtained by treating m-(aralkyl amido/imidoalkyl) benzoic acid hydrazides (3a-d) with carbon disulphide in alcoholic KOH and hydrazine hydrate, respectively. These triazole derivatives were employed in the synthesis of 5-[(3′-aralkyl amido/imidoalkyl) phenyl]-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines (6a-d). The newly synthesized compounds were evaluated for their antiviral activity against two animal viruses, namely, Japanese encephalitis virus (JEV) strain P20778 and herpes simplex virus-1

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34

Nakiwala, Rehema, Noopur Dasgupta, Rebecca Wilson, Erika I. Lutter, and Jeanne L. Bolliger. "Access to Substituted Tricyclic Heteroarenes by an Oxidative Cyclization Reaction and Their Antifungal Performance." Pharmaceuticals 18, no. 2 (2025): 249. https://doi.org/10.3390/ph18020249.

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Background/Objectives: Fungal pathogens are increasingly developing concerning resistance against the currently available antifungal drugs, which creates a constant demand for new antifungal agents. Methods: Here, we report the synthesis of C3,N4-substituted triazole derivatives containing a N4-(2-((4-methoxybenzyl)thio)phenyl) group. By selectively removing the 4-methoxybenzyl group, we were able to access the free thiol analogs which, under oxidative conditions, undergo a cyclization reaction yielding a C5-substituted benzo[4,5]thiazolo[2,3-c][1,2,4]triazole. We were able to show a broad fun

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35

Holla, Bantwala S., Channamata S. Prasanna, Boja Poojary, Mithun Ashok, Kottapalli S. Rao, and Kanakamajalu Shridhara. "Synthesis, Characterization and Antibacterial Studies of Some 1,2,4-Triazole Derivatives Containing a 6-Chloropyridin-3-yl methyl Moiety." Zeitschrift für Naturforschung B 61, no. 3 (2006): 334–38. http://dx.doi.org/10.1515/znb-2006-0315.

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Abstract5-(6-Chloropyridin-3-yl methyl)-4-phenyl-1,2,4-triazole-3-thiol (2) and 5-substituted-4-phenyl- 1,2,4-triazole-3-thiols (3) were synthesized. Alkylation and aminomethylation reactions of these triazoles were also carried out. Some of the newly synthesized compounds were screened for their antibacterial activities.

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36

Tashrifi, Zahra, Maryam Mohammadi-khanaposhtani, Mehdi Shafiee Ardestani, et al. "Design, Synthesis and In vitro Cytotoxicity of New 1,2,3-triazol- and Nitrostyrene Hybrids as Potent Anticancer Agents." Letters in Drug Design & Discovery 16, no. 2 (2018): 213–19. http://dx.doi.org/10.2174/1570180815666180427151830.

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Background: A new series of 1,2,3-triazol-nitrostyrene derivatives was designed, synthesized, and evaluated for cytotoxic activity against Hep-2 and L929 cell lines. </P><P> Methods: The synthetic procedure started from the functionalization of 4-hydroxybenzaldehyde with propargyl bromide and a subsequent click reaction to give 1,2,3-triazole derivatives. Then, the reaction of the mentioned derivatives with nitromethane led to the formation of the title compounds in excellent yields. Results: Most of the compounds exhibited better cytotoxic activity with respect to the standard dru

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37

Makhova, N. N., I. V. Ovchinnikov, A. S. Kulikov, S. I. Molotov, and E. L. Baryshnikova. "Monocyclic and cascade rearrangements of furoxans." Pure and Applied Chemistry 76, no. 9 (2004): 1691–703. http://dx.doi.org/10.1351/pac200476091691.

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Monocyclic rearrangements of azoles are extensively studied as alternative methods for the preparation of new heterocyclic systems. The present work is devoted to investigation of monocyclic and cascade rearrangements of 1,2,5-oxadiazole 2-oxide (furoxan) derivatives. It was found during investigations that rearrangements of furoxan ring had some peculiarities in comparison with analogous rearrangements of other azoles. Therefore, three different kinds of rearrangements were found. The first of them occurred through a dinitroso-ethylene intermediate and resulted in the synthesis of 1,2,3-triaz

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38

Aksyonova-Seliuk, I. I., O. I. Panasenko, and E. G. Knysh. "Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols." Farmatsevtychnyi zhurnal, no. 6 (August 14, 2018): 60–65. http://dx.doi.org/10.32352/0367-3057.6.16.03.

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Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and pu

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39

Sabzi, Noor Ali Hussein, and May Mohammed Jawad Al-Mudhafar. "Synthesis, characterization, and antimicrobial evaluation of new Schiff bases derived from vanillic acid conjugated to heterocyclic 4H-1,2,4-triazole-3-thiol." Pharmacia 70, no. (3) (2023): 657–63. https://doi.org/10.3897/pharmacia.70.e104579.

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A multistep synthesis was established for the preparation of a new vanillic acid-1, 2, 4-1triazole-3-thiol conjugate (4). Finally, several aromatized aldehydes reacted with compound (4) to produce Schiff bases derivatives (5–11). The purpose of this research is to prepare new vanillic acid derivatives with 1, 2, 4-triazole-3-thiol heterocyclic ring structures and to evaluate their antimicrobial activity in a preliminary assessment. Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance spectroscopy (<sup>1</sup>H-NMR) were used to verify the structures of the newly synthesize

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40

Yildirim, Nuri. "Synthesis of Novel 3-(4-tert-Butylphenyl)-5-Cylopropyl-4H-1,2,4-Triazole Derivatives with Antioxidative and Antimicrobial Activities." Letters in Drug Design & Discovery 17, no. 8 (2020): 954–64. http://dx.doi.org/10.2174/1570180817999200424073524.

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Background: In this work, new heterocyclic compounds containing 3-(4-tertbutylphenyl)- 5-cyclopropyl-4H-1,2,4-triazole ring were synthesized, starting from iminoester hydrochlorides and 4-tert-butylbenzhyrazide. Methods: Ethyl N-[(4-tert-butylphenyl)carbonyl]cyclopropanecarbohydrazonoate was used to synthesize 4-amino-3-(4-tert-butylphenyl)-5-cyclopropyl-4H-1,2,4-triazole, 3-(4-tert-butylphenyl)-5- cyclopropyl-4-(arylmethyleneamino)-4H-1,2,4-triazole, 3-(4-tert-butylphenyl)-5-cyclopropyl-4- (arylmethylamino)-4H-1,2,4-triazole and their phthalonitrile derivatives sequentially. Results: Seventee

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41

Journal, Baghdad Science. "Synthesis and Characterization of Some New Morpholine Derivatives." Baghdad Science Journal 13, no. 2 (2016): 253–65. http://dx.doi.org/10.21123/bsj.13.2.253-265.

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In this paper a new series of morpholine derivatives was prepared by reacting the morpholine with ethyl chloro acetate in the presence triethylamine as a catalyst in benzene gave morpholin-N-ethyl acetate(1) which reacted with hydrazine hydrate in ethanol, and gave morpholin-N-ethyl acetohydrazide (2) . Morpholin-N-aceto semithiocarbazide (3) were prepared by reacting compound(2) with ammonium thiocyanate , concentrated hydrochloric acid and ethanol as a solvent .Compound (3) reacted with sodium hydroxide and hydrochloric acid to give 5-(morpholin-N-methylene)-1H-1,2,4-triazole-3-thiol (4) .Th

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42

Tsyrenova, Biligma, and Valentine Nenajdenko. "Synthesis and Spectral Study of a New Family of 2,5-Diaryltriazoles Having Restricted Rotation of the 5-Aryl Substituent." Molecules 25, no. 3 (2020): 480. http://dx.doi.org/10.3390/molecules25030480.

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Efficient synthesis of 2,5-diaryl substituted 4-azido-1,2,3-triazoles by the reaction of sodium azide with dichlorosubstituted diazadienes was demonstrated. The optical properties of the prepared azidotriazoles were studied to reveal a luminescence maximum in the 360–420 nm region. To improve the luminescence quantum yields a family of 4-azido-1,2,3-triazoles bearing ortho-propargyloxy substituents in the 5 position was prepared. Subsequent intramolecular thermal cyclization permits to construct additional triazole fragment and obtain unique benzoxazocine derivatives condensed with two triazol

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43

Khan, Ayad Kareem. "Facile Synthesis, Characterization of New Quinazolinones with Different Azo Compounds, 1,2,3-Triazole Moieties and Evaluation Their Anti-bacterial Activity." Al-Mustansiriyah Journal of Science 28, no. 3 (2018): 122. http://dx.doi.org/10.23851/mjs.v28i3.180.

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In the present research, a series of some azo compounds (5-9) and 1,2,3-triazoles derived from 2-methyl quinazolin-4(3H)-one were synthesized successfully by stepwise routes includes the following: 3-amino-2-methylquinazolin-4(3H)-one (3) prepared firstly by conversion of 2-aminobenzoic acid into methyl 2-aminobenzoate (1) followed by reaction with acetic anhydride to form methyl -2-acetamidobenzoate (2). The amide then allowed reacting with hydrazine hydrate to give compound (3). Diazotization reaction with sodium nitrite in the presence of hydrochloric acid yield the 3-(chlorodiazenyl)-2-met

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44

Nurhan G mr k o lu, Nurhan G. mr k. o. lu, and Muhammad Imran and Inam Iqbal Muhammad Imran and Inam Iqbal. "Synthesıs and Characterızatıon of New Trıazole and Coumarın-Derived Heterocyclıc Compounds Part I." Journal of the chemical society of pakistan 41, no. 6 (2019): 1097. http://dx.doi.org/10.52568/000830/jcsp/41.06.2019.

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Synthesis of ethyl ester of acetic acid containing 5-oxo-[1,2,4] triazole ring (2) was achieved by the condensation of 3-substituted-4-amino-1H-1,2,4-triazol-5(4H)-one (1) with ethyl bromoacetate in basic medium. Compound 2, was then further reacted with hydrazine hydrate to form acid hydrazide, which is 2-(4-amino-3-substituted-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)acetohydrazide (3). Compound 3 was later treated with three different diverse coumarin aldehydes (6, 12, 18) resulted in the formation of arylidene hydrazides as cis–trans conformers (7, 8, 13, 14, 19, 20). In conclusion, we synt

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45

Nahlé, A., R. Salim, F. El Hajjaji, et al. "Novel triazole derivatives as ecological corrosion inhibitors for mild steel in 1.0 M HCl: experimental & theoretical approach." RSC Advances 11, no. 7 (2021): 4147–62. http://dx.doi.org/10.1039/d0ra09679b.

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The present paper illustrates the investigation of two novel ecological triazole derivative corrosion inhibitors, namely ethyl 2-(4-phenyl-1H-1,2,3-triazol-1-yl) acetate [Tria-CO<sub>2</sub>Et], and 2-(4-phenyl-1H-1,2,3-triazol-1-yl) acetohydrazide [Tria-CONHNH<sub>2</sub>].

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46

H. Abed Elwahab Al-Somaidai, Gazwan. "Synthesis and study the biological activity of some new derivatives of 1,2,4-triazole compounds." Tikrit Journal of Pharmaceutical Sciences 1, no. 1 (2023): 64–70. http://dx.doi.org/10.25130/tjphs.2005.1.8.64.70.

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Some derivatives of triazoles have been synthesized . These derivatives (Schiff's bases) were resulted from the reaction of (3-( 4-methoxy phenyl)-4-amino-5 mercapto-1,2,4-triazole and the corresponding substituted benzaldehydes in presence of glacial acetic acid . The chemical structures of the products were characterized by IR and UV spectra, elemental analysis C.H.N and the biological activity were studied against different kinds of bacteria.

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47

Danilkina, Natalia A., Nina S. Bukhtiiarova, Anastasia I. Govdi, et al. "Synthesis and Properties of 6-Aryl-4-azidocinnolines and 6-Aryl-4-(1,2,3-1H-triazol-1-yl)cinnolines." Molecules 24, no. 13 (2019): 2386. http://dx.doi.org/10.3390/molecules24132386.

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An efficient approach towards the synthesis of 6-aryl-4-azidocinnolines was developed with the aim of exploring the photophysical properties of 6-aryl-4-azidocinnolines and their click reaction products with alkynes, 6-aryl-4-(1,2,3-1H-triazol-1-yl)cinnolines. The synthetic route is based on the Richter-type cyclization of 2-ethynyl-4-aryltriazenes with the formation of 4-bromo-6-arylcinnolines and nucleophilic substitution of a bromine atom with an azide functional group. The developed synthetic approach is tolerant to variations of functional groups on the aryl moiety. The resulting azidocin

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48

Bihdan, O. A., V. V. Parchenko, and B. V. Gutyj. "Some transformations in a series of 4-amino-1,2,4-triazole-3-thion derivatives." Current issues in pharmacy and medicine: science and practice 17, no. 2 (2024): 103–7. http://dx.doi.org/10.14739/2409-2932.2024.2.298780.

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The continuous improvement of synthesis methods enables the optimization of the process for developing and obtaining target products of chemical transformation. Derivatives of 1,2,4-triazole-3-thiol present a convenient object for chemical transformation, facilitating the creation of promising biologically active compounds. Combining the structure of this heterocyclic system with pharmacophore fragments of different natures allows for more effective work on the development of molecules with high pharmacological potential. To implement this strategy, 2-,3-,4-fluorophenyl-4-amino-1,2,4-triazol-3

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Basireddy, Avanthi, Tejeswara Rao Allaka, Avekananda Reddy Allam, Sudhakar Reddy Baddam, Sravanthi Basireddy, and Pilli Veera Venkata Nanda Kishore. "Quinolone Tethered 1,2,3-triazole Conjugates: Design, Synthesis, and Computational Docking Studies on New Heterocycles as Potent Antimicrobial Targets." Current Organic Chemistry 27, no. 21 (2023): 1882–95. http://dx.doi.org/10.2174/0113852728276712231123111714.

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Abstract: The synthesis and biological properties of molecules simultaneously comprising various heterocycles, such as fused 2-quinolones and 1,2,3-triazoles, have been evaluated as a part of our ongoing research in medicinal and organic chemistry. We were successful in developing a synthetic procedure for 1,2,3-triazole substituted quinolone derivatives. Infrared, proton, and carbon nuclear magnetic resonance, mass spectroscopy and elemental analysis were used to characterise the structures of the recently synthesised triazole derivatives. From screening results, all the compounds demonstrate

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ARCHANA, JYOTI SRIVASTAVA, SWARUP SANJAY, K. SAXENA V., and L. CHOWDHURY B. "Synthesis and Antiviral Activity of 4-Aryl-5- (3,5-dinitrobenzoyl)-3-mercapto-N-arylidene-acetylhydrazinotriazoles." Journal of Indian Chemical Society Vol. 68, Feb 1991 (1991): 103–4. https://doi.org/10.5281/zenodo.6134289.

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Chemistry Department, Lucknow University, Lucknow-226 007 Department of Virology, Central Drug Research Institute, Lucknow-226 007 <em>Manuscript received 23 July 1990, revised 29 November 1990, accepted 14 January 1991</em> VARIOUS antiviral activities have been found to abe associated with the triazole derivatives. Some cylated 1,2,4-triazole derivatives are known to possess antiviral activity. 4-Aryl-3-(4-chlorophenylthiomethyl)- 5-mercaptoacetyl. <em>N</em>- arylureido - 1,2,4- triazoles have shown antiviral activity against tobacco mosaic virus. These finding

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