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Journal articles on the topic 'Thiosemicarbazone derivatives'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Kozakiewicz, Dariusz. "TAUTOMERYCZNA TRANSFORMACJA W TIOSEMIKARBAZONACH POCHODNYCH ALFA-AMINOKETONÓW NOWĄ METODĄ SYNTEZY POCHODNYCH HYDROKSYTIOSEMIKARBAZONÓW, JAKO ZWIĄZKÓW O POTENCJALNEJ AKTYWNOŚCI BIOLOGICZNEJ." Wiadomości Chemiczne 78, no. 11 (2024): 1749–78. https://doi.org/10.53584/wiadchem.2024.11.15.

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Thiosemicarbazones are an important pharmacophore that gives biological activity to chemical molecules, which is why these compounds are of great interest in the pharmaceutical industry. During research on the possibility of obtaining alpha-aminotiosemicarbazones by reacting alpha-aminoketones with thiosemicarbazide, the phenomenon of rearrangement of the thiosemicarbazide group with the cleavage of the appropriate amine and the formation of a neighboring hydroxyl group was observed. This publication describes this reaction as a new method for obtaining hydroxy-thiosemicarbazone derivatives, w

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2

Rekiba, Nawel, Abdelmadjid Benmohammed, Sofiane Khanoussi, Ayada Djafri, and Jérôme Thibonnet. "Synthesis and Characterization of Novel Thiazolidinones and Thioxothiazolidinones Derived from Substituted Indole." Molbank 2021, no. 4 (2021): M1284. http://dx.doi.org/10.3390/m1284.

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Based on recent discoveries concerning the numerous biological properties of thiazolidinones and thiosemicarbazones, new N-substituted heterocyclic derivatives have been designed by combining the indole ring with thioxothiazolidinone, thiazolidinone or thiosemicarbazone. Thus, a series of new thioxothiazolidinone, thiazolidinone, or thiosemicarbazone derivatives bearing indole-based moiety have been designed, synthesized, and developed in good yields.

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3

Al-Harbi, Reem A. K., Marwa A. M. Sh El-Sharief, and Samir Y. Abbas. "Synthesis of New of 4-Thiazolidinone and Thiazole Derivatives Containing Coumarin Moiety with Antimicrobial Activity." Acta Chimica Slovenica 70, no. 4 (2023): 500–508. http://dx.doi.org/10.17344/acsi.2023.8281.

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Synthesizing hybrid molecules is one of the best manners to achieve novel promising agents. Consequently, series of new thiazoles having coumarin nucleus were synthesized from 3-acetylcoumarin thiosemicarbazones. Cyclization of thiosemicarbazone derivatives with ethyl 2-chloroacetate, 1-chloropropan-2-one and 2-bromo-1-phenylethanone afforded the corresponding 4-thiazolidinones, 4-methylthiazoles and 4-phenylthiazoles, respectively. The expected antimicrobial proprieties for the synthesized thiosemicarbazone and thiazole derivatives were investigated. The thiosemicarbazones and thiazolidin-4-o

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4

Santos, Felipe R. S., Jéssica T. Andrade, Carla D. F. Sousa, et al. "Synthesis and Evaluation of the in vitro Antimicrobial Activity of Triazoles, Morpholines and Thiosemicarbazones." Medicinal Chemistry 15, no. 1 (2019): 38–50. http://dx.doi.org/10.2174/1573406414666180730111954.

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Background: Microbial infections is a global public health problem. The aim of this work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and thiosemicarbazones. </P><P> Methods: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde as starting materials. The antimicrobial activity of these compounds against bacteria and yeast was evaluated by the broth microdilution method. Results: The proposed route for synthesis gave high to moderate yields, moreover these compounds were successfully characterized by 1H NMR

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5

Hernández, Wilfredo, Fernando Carrasco, Abraham Vaisberg, et al. "Novel Thiosemicarbazone Derivatives from Furan-2-Carbaldehyde: Synthesis, Characterization, Crystal Structures, and Antibacterial, Antifungal, Antioxidant, and Antitumor Activities." Journal of Chemistry 2023 (September 14, 2023): 1–20. http://dx.doi.org/10.1155/2023/5413236.

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Ten new thiosemicarbazone derivatives, furan-2-carbaldehyde thiosemicarbazone (1), 3-methyl-furan-2-carbaldehyde thiosemicarbazone (2), 5-hydroxymethyl-furan-2-carbaldehyde thiosemicarbazone (3), 5-trifluoromethyl-furan-2-carbaldehyde thiosemicarbazone (4), 5-nitro-furan-2-carbaldehyde thiosemicarbazone (5), 5-phenyl-furan-2-carbaldehyde thiosemicarbazone (6), 5-(2-fluorophenyl)-furan-2-carbaldehyde thiosemicarbazone (7), 5-(4-methoxyphenyl)-furan-2-carbaldehyde thiosemicarbazone (8), 5-(1-naphthyl)-furan-2-carbaldehyde thiosemicarbazone (9), and 5-(1H-Pyrazol-5-yl)-furan-2-carbaldehyde thiose

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6

Martínez-Estévez, Mónica, Soledad García-Fontán, Saray Argibay-Otero, Inmaculada Prieto, and Ezequiel M. Vázquez-López. "Synthesis, Characterization, and Cytotoxicity Studies of N-(4-Methoxybenzyl) Thiosemicarbazone Derivatives and Their Ruthenium(II)-p-cymene Complexes." Molecules 27, no. 22 (2022): 7976. http://dx.doi.org/10.3390/molecules27227976.

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The reaction of [Ru2Cl2(μ-Cl)2(η6-p-cymene)2] with two thiosemicarbazones obtained by the condensation of N-(4-methoxybenzyl) thiosemicarbazide and 1,4-hydroxy-3-methoxyphenyl)ethan-1-one (HL1) or 2-fluoro-4-hydroxybenzaldehyde (HL2) was studied. The cationic complexes of formula [RuCl(η6-p-cymene)(HL)]+ were isolated as solid chloride and trifluoromethylsulfate (TfO) salts. A study of the solid state and NMR spectra suggests the presence in the material of two isomers that differ in the configuration in the iminic bond, C2=N3, of the coordinated thiosemicarbazone in the triflate salts and onl

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7

Hernández, Wilfredo, Fernando Carrasco, Abraham Vaisberg, et al. "Synthesis, Spectroscopic Characterization, Structural Studies, and In Vitro Antitumor Activities of Pyridine-3-carbaldehyde Thiosemicarbazone Derivatives." Journal of Chemistry 2020 (September 14, 2020): 1–12. http://dx.doi.org/10.1155/2020/2960165.

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Eight new thiosemicarbazone derivatives, 6-(1-trifluoroethoxy)pyridine-3-carbaldehyde thiosemicarbazone (1), 6-(4′-fluorophenyl)pyridine-3-carbaldehyde thiosemicarbazone (2), 5-chloro-pyridine-3-carbaldehyde thiosemicarbazone (3), 2-chloro-5-bromo-pyridine-3-carbaldehyde thiosemicarbazone (4), 6-(3′,4′-dimethoxyphenyl)pyridine-3-carbaldehyde thiosemicarbazone (5), 2-chloro-5-fluor-pyridine-3-carbaldehyde thiosemicarbazone, (6), 5-iodo-pyridine-3-carbaldehyde thiosemicarbazone (7), and 6-(3′,5′-dichlorophenyl)pyridine-3-carbaldehyde thiosemicarbazone (8) were synthesized, from the reaction of t

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8

Ashok, N. Patange*1 Ramesh G.Paloti2 Ramesh N.Zade3 Kushal M.Mude4 &. Bhupesh M.Mude5. "DESIGN, SYNTHESIS AND CHARACTERISATION OF SOME SEMICARBAZONE AND THIOSEMICARBAZONE DERIVED FROM 3-PHENYLQUINAZOLINE-2, 4(1H, 3H)-DIONE." GLOBAL JOURNAL OF ENGINEERING SCIENCE AND RESEARCHES 5, no. 4 (2018): 10–14. https://doi.org/10.5281/zenodo.1211485.

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This paper presents the synthesis and characterizations of some semicarbazone and thiosemicarbazone derivatives of3-phenylquinazoline-2,4(1H,3H)-dione. All compounds reported here had been characterised by<sup>1</sup>H NMR and IR spectral studies and elemental analysis. semicarbazone and thiosemicarbazone derivatives of 3-phenylquinazoline-2,4(1H,3H)-dionewere prepared by treating mixture of phenyl isocyanates and anthanilic acid in ethanol to get 3-phenylquinazoline-2,4(1H,3H)-dionewhich will then condense with substituted4-chloro/bromo/iodoAcetophenones in ethanolto form the chalcones .this

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9

Czylkowska, Agnieszka, Monika Pitucha, Anita Raducka, et al. "Thiosemicarbazone-Based Compounds: A Promising Scaffold for Developing Antibacterial, Antioxidant, and Anticancer Therapeutics." Molecules 30, no. 1 (2024): 129. https://doi.org/10.3390/molecules30010129.

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This paper presents the synthesis and characterization of new thiosemicarbazone derivatives with potential applications as antibacterial, antioxidant and anticancer agents. Six thiosemicarbazone derivatives (L–L5) were synthesized by reacting an appropriate thiosemicarbazide derivative with 2-pyridinecarboxaldehyde. The structures of the obtained compounds were confirmed using mass spectrometry, infrared spectroscopy, and NMR spectroscopy. Antibacterial activity was evaluated by using the microdilution method, determining the minimum inhibitory concentration (MIC) against a panel of Gram-posit

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10

Kamal, Kishor Verma, and Kumar Verma Suresh. "Microwave Assisted Synthesis, Spectroscopic Characterization and Antimicrobial Activities of Co(II) Complexes Containing Biologically Active Thiosemicarbazone Derivatives." Chemistry Research Journal 6, no. 5 (2021): 80–86. https://doi.org/10.5281/zenodo.11805215.

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<strong>Abstract </strong>In present study two thiosemicarbazone ligands i.e. 4HAT and 3NBT and their  novel Cobal(II) aryl thiosemicarbazones complexes having the general composition [Co(L<sub>1</sub>)<sub>2</sub>Cl<sub>2</sub>], [Co(L<sub>2</sub>)<sub>2</sub>Cl<sub>2</sub>],{where L<sub>1</sub>= 4-Hydroxyacetophenone thiosemicarbazones (4HAT), L<sub>2 </sub>= 3-Nitrobenzaldehyde thiosemicarbazones (3NBT), have been synthesized by the reaction of thiosemicarbazide with substituted aromatic aldehydes and ketones by conventional heating as well as microwave irradiations method followed by

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11

Nagoor Meeran M and Narayanan Ravisankar. "Synthesis and characterization of substituted acetophenone-4, 4-dimethyl-3-thiosemicarbazone derivatives with an evaluation of antimicrobial and antioxidant activities." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (2020): 7192–97. http://dx.doi.org/10.26452/ijrps.v11i4.3844.

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Thiosemicarbazones are organic compounds; these are widely used in the medical field. It is primarily in the manufacture of pharmaceutical drugs and bio molecules. These compounds have the azomethine functional group (-N=CH-) used to derive organic open chain and heterocyclic compounds. Thiosemicarbazones are similar to semicarbazones, and carbonyl group oxygen is replaced by sulphur. Thiosemicarbazone contains nitrogen and sulfur atoms, so they are used as ligands in coordination chemistry and form metal complexes. Thiosemicarbazone and its metal complexes are used in a variety of ways. It is

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12

Kuruca, Serap Erdem, Nilgun Karali, Beyza Cetin, Sabriye Karadenizli, and Zeynep Karakas. "The Antileukemic Potential of New Derivatives of 5-Fluoro-1H-Indole-2,3-Dione-3-Thiosemicarbazone on in Vitro Cell Lines." Blood 112, no. 11 (2008): 5055. http://dx.doi.org/10.1182/blood.v112.11.5055.5055.

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Abstract 1H-Indole-2,3-dione (isatin) is an endogenous compound identified in many organisms, possesses a wide range of biological activities. Biological properties of isatin include a range of actions in brain and offer protection against certain types of infections. This molecule has a versatile moiety that displays diverse biological activities, including anticancer activity. The discovery of numerous biologically active 3-substituted 2-indolinones led in the past decade to extensive synthesis of related compounds and as a result, anticancer agents were developed. In particular, among the 5

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13

Shadmani, Yasaman, Yaghoub Pourshojaei, Somayyeh Karami-Mohajeri, Bagher Amirheidari, and Motahareh Sadeghzadeh. "Synthesis of thiosemicarbazone derivatives and evaluation of their cytotoxicity with emphasis on ferroptosis biomarkers; an in vitro study." Research in Pharmaceutical Sciences 20, no. 3 (2025): 445–55. https://doi.org/10.4103/rps.rps_120_24.

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Background and purpose: This study aimed to evaluate the cytotoxicity of synthesized thiosemicarbazone derivatives, particularly on biomarkers associated with ferroptosis. Experimental approach: Thiosemicarbazone derivatives (C1-C5) were synthesized by condensation between thiosemicarbazide and the corresponding benzaldehyde derivatives. The compounds were characterized using IR spectroscopy and H/C NMR spectroscopy. To evaluate their biological activity, PC-12 cells were cultured in DMEM/MEM medium supplemented with 10% bovine serum albumin. Cell viability was assessed using the MTT assay, wh

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14

García, Cybele C., Beatriz N. Brousse, Marla J. Carlucci, et al. "Inhibitory Effect of Thiosemicarbazone Derivatives on Junin Virus Replication In Vitro." Antiviral Chemistry and Chemotherapy 14, no. 2 (2003): 99–105. http://dx.doi.org/10.1177/095632020301400205.

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The inhibitory effect of several thiosemicarbazones (TSCs), synthesized from aromatic ketones and terpenones, and their heterocyclic thiadiazoline (TDZ) derivatives, was investigated against Junin virus (JUNV), an arenavirus agent of Argentine haemorrhagic fever. From the 25 compounds tested, six compounds belonging to the TSC group were found to be selective inhibitors of JUNV, with EC50 values determined by a virus yield inhibition assay in the range 3.4–12.5 μM, and selectivity indices greater than 10. By contrast, most of the TDZs obtained by heterocyclization of the TSCs were not active a

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15

Zhang, H. H., C. K. Qin, Y. Chen, and Z. Zhang. "Inhibition behaviour of mild steel by three new benzaldehyde thiosemicarbazone derivatives in 0.5 M H 2 SO 4 : experimental and computational study." Royal Society Open Science 6, no. 8 (2019): 190192. http://dx.doi.org/10.1098/rsos.190192.

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Three new benzaldehyde thiosemicarbazone derivatives namely benzaldehyde thiosemicarbazone (BST), 4-carboxyl benzaldehyde thiosemicarbazone (PBST) and 2-carboxyl benzaldehyde thiosemicarbazone (OCT) were synthesized and their inhibition effects on mild steel corrosion in 0.5 M H 2 SO 4 solution were studied systematically using gravimetric and electrochemical measurements. Weight loss results revealed that PBST exhibited the highest inhibition efficiency of 96.6% among the investigated compounds when the concentration was 300 µM. The analysis of polarization curves indicated that the three ben

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16

El-mahdy, Kamelia, Azza El-Kazak, Mohamed Abdel-Megid, Magdy Seada, and Osama Farouk. "Synthesis, Characterization and Biological Evaluation of some New Thieno[2,3-d]Pyrimidine Derivatives." JOURNAL OF ADVANCES IN CHEMISTRY 5, no. 1 (2009): 581–91. http://dx.doi.org/10.24297/jac.v5i1.937.

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10-Oxo-4,6,7,8,9,10-hexahydroprazolo[1,5-a][1]benzothieno[2,3-d]pyrimidine-3-carbaldehyde (2) was prepared by Vilsmeier-Haack reaction of 3-amino-2-methyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one (1). Reaction of carbaldehyde derivative 2 with malononitrile afforded arylidene malononitrile 3. Cyclization of the latter compound with thiourea yielded pyrimidinethione 4. Interaction of carbaldehyde derivative 2 in presence of thiourea with keto- compounds such as ethyl acetoacetate, or acetylacetone, or dimedone or ethyl cyanoacetate gave pyrimidine derivatives 5-8. Hydrazinolys

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17

Er, Mustafa, Ayşe Şahin, and Hakan Tahtacı. "Synthesis and Characterization of Novel 1,3-Thiazole and 2-Amino-1,3,4-Thiadiazole Derivatives." Macedonian Journal of Chemistry and Chemical Engineering 33, no. 2 (2014): 189. http://dx.doi.org/10.20450/mjcce.2014.522.

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<p>Thiosemicarbazone derivatives <strong>3a–e</strong> were synthesized by the reaction of various aldehydes<strong> 1a–e</strong> with 4-methyl thiosemicarbazide <strong>2</strong> in 78% to 90% yield. Then, the thiazole moieties of the target materials <strong>5a–e</strong> were obtained in high yields (71–93%) using the Hantzsch reaction utilizing thiosemicarbazone derivatives <strong>3a–e</strong> with ethyl-2-chloroacetoacetic ester. The substituted nitrile derivatives <strong>7a–e</strong> were obtained in mode

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18

K., H. Popat, H. Purohit D., T. Chovatia P., and S. Joshi H. "Synthesis of some thiosemicarbazone and oxirane derivatives as potent antitubercular agents." Journal of Indian Chemical Society Vol. 82, Oct 2005 (2005): 940–41. https://doi.org/10.5281/zenodo.5827255.

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Department of Chemistry, Saurashtra University, Rajkot-360 005, India <em>E-mail</em> : drhsjoshi@yahoo.com                            <em>Fax</em>: 91-281-2578512 <em>Manuscript received 13 August 2004, revised 7 July 2005, accepted 14 July 2005</em> Condensation of thiosemicarbazide with 1-aryl-3-(3'-chlorophenyl)-2-propene-1-ones (la-j) afforded corresponding 4-α( 3'-chlorostyryl)-benzylidene-thiosemicarbazones (2a-j) and the compounds (1a-j) on reaction with alkaline H<sub>2</sub>O<sub>2</sub> gave 3-(3&#39

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19

Verochkina, E. A., N. V. Vchislo, L. I. Larina, and E. A. Titov. "Synthesis and characterization of 2,5-dibutylthio-2,3-dihydro-2-formyl-4H-pyran thiosemicarbazones and their copper complexes." Proceedings of Universities. Applied Chemistry and Biotechnology 12, no. 1 (2022): 167–72. http://dx.doi.org/10.21285/2227-2925-2022-12-1-167-172.

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Previously unknown derivatives of thiosemicarbazide were obtained in high yields by the condensation reaction of 2,5-dibutylthio-2,3-dihydro-2-formyl-4H-pyran with 4-phenylthiosemicarbazide or thiosemicarbazide when boiling in EtOH. The reaction products are represented by colored oils. Cu(II) complexes based on 2,5-dibutylthio-2,3-dihydro-2-formyl-4H-pyran carbazones were synthesized by their interaction with copper (II) chloride. All these complexes are soluble in dimethylformamide (DMF) and dimethyl sulfoxide (DMSO) and, according to elemental analysis, have a 1:1 metal-ligand stoichiometry

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20

Sutradhar, Ranajit Kumar, Aongchainu Marma, and Md Emdad Hossain. "Synthesis, Bioactivity Screening and Docking Analysis of Thiazole Derivatives Containing Quinoline Moieties." Oriental Journal Of Chemistry 40, no. 5 (2024): 1297–305. http://dx.doi.org/10.13005/ojc/400511.

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A new series of quinoline-thiazole compounds (1b-3b) were synthesized by two step reaction where thiosemicarbazone derivatives (1a-3a) were obtained from quinolinecarbaldehyde and thiosemicarbazide. The final products (1b-3b) were synthesized from thiosemicarbazone and 3-chloroacetylacetone. Characterizations of all synthesized compounds (1a-3a, 1b-3b) were performed by IR, Proton and Carbon-13 NMR spectroscopic methods. In vitro antimicrobial studies of thiazole derivatives (1b-3b) were screened by agar disc diffusion method. Compounds 1b and 3b revealed significant antibacterial effects agai

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21

Yadav, Vijay Kumar, Meena Bhandari, and Satbir Singh. "GREEN SYNTHESIS AND ANTIMICROBIAL EVALUATION OF SOME THIOSEMICARBAZONE AND SEMICARBAZONE DERIVATIVES." RASAYAN Journal of Chemistry 17, no. 04 (2024): 1727–31. http://dx.doi.org/10.31788/rjc.2024.1748967.

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The interaction of substituted pyridine carboxaldehyde with thiosemicarbazide and semicarbazide via a greener approach resulted in the synthesis of thiosemicarbazone and semicarbazone derivatives; respectively. The resultant compounds were synthesized in aqueous media and were characterized by FTIR and 1H-NMR spectral studies. The antimicrobial evaluation of the final compounds has proven that they are active against the strains (S. aureus, P. aeruginosa, A. niger, and C. glabrata) incorporating the microdilution method.

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22

Orsoni, Nicolò, Francesca Degola, Luca Nerva, et al. "Double Gamers—Can Modified Natural Regulators of Higher Plants Act as Antagonists against Phytopathogens? The Case of Jasmonic Acid Derivatives." International Journal of Molecular Sciences 21, no. 22 (2020): 8681. http://dx.doi.org/10.3390/ijms21228681.

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As key players in biotic stress response of plants, jasmonic acid (JA) and its derivatives cover a specific and prominent role in pathogens-mediated signaling and hence are promising candidates for a sustainable management of phytopathogenic fungi. Recently, JA directed antimicrobial effects on plant pathogens has been suggested, supporting the theory of oxylipins as double gamers in plant-pathogen interaction. Based on these premises, six derivatives (dihydrojasmone and cis-jasmone, two thiosemicarbazonic derivatives and their corresponding complexes with copper) have been evaluated against 1

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23

Salem, Mohamed A., Samir Y. Abbas, Marwa A. M. Sh El-Sharief, et al. "Novel Structural Hybrids of Pyrrole and Thiazole Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities." Acta Chimica Slovenica 68, no. 4 (2021): 990–96. http://dx.doi.org/10.17344/acsi.2021.6980.

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One of the best ways to design new biocidal agents is synthesizing hybrid molecules by combining two or more bioactive moieties in a single molecular scaffold. So, new series of pyrroles bearing a thiazole moiety were synthesized using 1-methyl-1H-pyrrole-2-carbaldehyde thiosemicarbazones 1a–c. Cyclization of thiosemicarbazone derivatives 1a–c with ethyl chloroacetate, ethyl 2-chloropropanoate, chloroacetone and phenacyl bromide afforded the corresponding thiazolidin-4-ones 2a–c, 5-methylthiazolidin-4-ones 3a–c, 4-methyl-2,3-dihydrothiazoles 4a–c, and 4-phenyl-2,3-dihydrothiazoles 5a–c, respec

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24

Sunitha, K., Smitha Nair, and P. Palanisamy. "Synthesis, Characterization and Biological Evaluation of Some Novel Azo-Imine Compounds." Asian Journal of Chemistry 34, no. 3 (2022): 663–67. http://dx.doi.org/10.14233/ajchem.2022.23591.

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The oxidative cyclization of thiosemicarbazone (III) synthesized from reaction between substituted aryl aldehydes (I) with thiosemicarbazide (II) was done using ferric chloride as oxidative agent to get 2-amino-5-phenyl-1,3,4-thiadiazole (IV). 2-Amino-5-phenyl-1,3,4-thiadiazole was introduced in condensation reactions with substituted aldehydes to obtain benzylidene imine derivatives (VI)1-5. Further these were treated with sulphanilic acid to give new 2-{[5-phenyl-1,3,4-thiadiazole-2-imino] substituted benzene}diazenyl benzene sulfonic acid derivatives (VII)1-5. These derivatives were further

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25

Koshelev, Vladimir N., Olga V. Primerova, Stepan V. Vorobyev, Anna S. Stupnikova, and Ludmila V. Ivanova. "Synthesis and Antioxidant Activity of Novel Thiazole and Thiazolidinone Derivatives with Phenolic Fragments." Applied Sciences 13, no. 24 (2023): 13112. http://dx.doi.org/10.3390/app132413112.

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In this work, a series of thiosemicarbazones with phenol fragments were used as starting compounds for the synthesis of new effective antioxidants containing both a phenol substituent and a heterocyclic fragment: thiazole and thiazolidinone. To determine the most stable conformation of thiosemicarbazone, a potential energy scan was used, along with NOESY NMR spectroscopy data. A number of thiazole derivatives were obtained due the interaction of thiosemicarbazones with several bromoketones: bromoacetophenone, bromodimedone, and bromoacetylcoumarin. The product yields varied from 71 to 94%. Thi

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Kaplancıklı, Zafer Asım, Mehlika Dilek Altıntop, Belgin Sever, Zerrin Cantürk, and Ahmet Özdemir. "Synthesis andIn VitroEvaluation of New Thiosemicarbazone Derivatives as Potential Antimicrobial Agents." Journal of Chemistry 2016 (2016): 1–7. http://dx.doi.org/10.1155/2016/1692540.

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In an effort to develop potent antimicrobial agents, new thiosemicarbazone derivatives were synthesizedviathe reaction of 4-[4-(trifluoromethyl)phenyl]thiosemicarbazide with aromatic aldehydes. The compounds were evaluated for their inhibitory effects on pathogenic bacteria and yeasts using the CLSI broth microdilution method. Microplate Alamar Blue Assay was also carried out to determine the antimycobacterial activities of the compounds againstMycobacterium tuberculosisH37Rv. Among these derivatives, compounds5and11were more effective againstEnterococcus faecalis(ATCC 29212) than chlorampheni

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Pitucha, Monika, Agnieszka Korga-Plewko, Agnieszka Czylkowska, et al. "Influence of Complexation of Thiosemicarbazone Derivatives with Cu (II) Ions on Their Antitumor Activity against Melanoma Cells." International Journal of Molecular Sciences 22, no. 6 (2021): 3104. http://dx.doi.org/10.3390/ijms22063104.

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A series of thiosemicarbazone derivatives was prepared and their anti-tumor activity in vitro was tested. The X-ray investigation performed for compounds T2, T3 and T5 confirmed the synthesis pathway and assumed molecular structures of analyzed thiosemicarbazones. The conformational preferences of the thiosemicarbazone system were characterized using theoretical calculations by AM1 method. Selected compounds were converted into complexes of Cu (II) ions. The effect of complexing on anti-tumor activity has been investigated. The copper(II) complexes, with Schiff bases T1, T10, T12, T13, and T16

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Roque Marques, Karla Mirella, Maria Rodrigues do Desterro, Sandrine Maria de Arruda, et al. "5-Nitro-Thiophene-Thiosemicarbazone Derivatives Present Antitumor Activity Mediated by Apoptosis and DNA Intercalation." Current Topics in Medicinal Chemistry 19, no. 13 (2019): 1075–91. http://dx.doi.org/10.2174/1568026619666190621120304.

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Background: Considering the need for the development of new antitumor drugs, associated with the great antitumor potential of thiophene and thiosemicarbazonic derivatives, in this work we promote molecular hybridization approach to synthesize new compounds with increased anticancer activity. Objective: Investigate the antitumor activity and their likely mechanisms of action of a series of N-substituted 2-(5-nitro-thiophene)-thiosemicarbazone derivatives. Methods: Methods were performed in vitro (cytotoxicity, cell cycle progression, morphological analysis, mitochondrial membrane potential eval

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Silva, Bianca N. M., Policarpo A. Sales Junior, Alvaro J. Romanha, et al. "Synthesis of New Thiosemicarbazones and Semicarbazones Containing the 1,2,3-1H-triazole-isatin Scaffold: Trypanocidal, Cytotoxicity, Electrochemical Assays, and Molecular Docking." Medicinal Chemistry 15, no. 3 (2019): 240–56. http://dx.doi.org/10.2174/1573406414666180912120502.

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Background: Chagas disease, also known as American trypanosomiasis, is classified as one of the 17 most important neglected diseases by the World Health Organization. The only drugs with proven efficacy against Chagas disease are benznidazole and nifurtimox, however both show adverse effects, poor clinical efficacy, and development of resistance. For these reasons, the search for new effective chemical entities is a challenge to research groups and the pharmaceutical industry. Objective: Synthesis and evaluation of antitrypanosomal activities of a series of thiosemicarbazones and semicarbazone

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Pósa, Vivien, Alessia Stefanelli, Julia H. Bormio Nunes, et al. "Thiosemicarbazone Derivatives Developed to Overcome COTI-2 Resistance." Cancers 14, no. 18 (2022): 4455. http://dx.doi.org/10.3390/cancers14184455.

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COTI-2 is currently being evaluated in a phase I clinical trial for the treatment of gynecological and other solid cancers. As a thiosemicarbazone, this compound contains an N,N,S-chelating moiety and is, therefore, expected to bind endogenous metal ions. However, besides zinc, the metal interaction properties of COTI-2 have not been investigated in detail so far. This is unexpected, as we have recently shown that COTI-2 forms stable ternary complexes with copper and glutathione, which renders this drug a substrate for the resistance efflux transporter ABCC1. Herein, the complex formation of C

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Wakodkar, Rohit R., Mazahar Farooqui, Pravin Kulkarni, and Deepak D. Kayande. "Synthesis and Biological Activity of Some Thiosemicarbazide." Asian Journal of Organic & Medicinal Chemistry 4, no. 4 (2019): 228–31. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p206.

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In this paper, thiosemicarbazone derivatives have been prepared from substituted aromatic aldehyde and thiosemicarbazide in presence of sodium chloride. This method is an efficient, mild, inexpensive, non-toxic and environment benign catalyst. This protocol includes the reaction followed by using sodium chloride to accelerate the reaction in aqueous ethanol. The structure of synthesized compounds were determined by IR, 1H NMR, 13C NMR and mass spectroscopies as well as the compounds were also screened for antibacterial and antifungal activity against certain Gram-negative and Gram-positive bac

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Dipke, S. S., and J. R. Gujarathi. "4(N)-ARYL/ALKYL SUBSTITUTED THIOSEMICARBAZONE DERIVED METAL COMPLEXES, THEIR SPECTRAL AND BIOCHEMICAL STUDIES: A REVIEW." International Journal of Advanced Research 12, no. 11 (2024): 584–636. https://doi.org/10.21474/ijar01/19870.

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N(4)-alkyl/aryl substituted thiosemicarbazones and their metal complexes show significantly enhanced biochemical properties than well-known standard drugs. In this review, we extensively focused on the synthesis, biological applications, and structural characterization of the aforementioned compounds over the past decade. A detailed description of the structures of thiosemicarbazone derivatives substituted at the N(4)-position and their metal complexes is presented here. The structures of the compounds were elucidated with respect to their bonding interactions with metal ions and their geometr

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Sibuh, Belay Zeleke, Piyush Kumar Gupta, Pankaj Taneja, et al. "Synthesis, In Silico Study, and Anti-Cancer Activity of Thiosemicarbazone Derivatives." Biomedicines 9, no. 10 (2021): 1375. http://dx.doi.org/10.3390/biomedicines9101375.

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Thiosemicarbazones are known for their biological and pharmacological activities. In this study, we have synthesized and characterized 3-Methoxybenzaldehyde thiosemicarbazone (3-MBTSc) and 4-Nitrobenzaldehyde thiosemicarbazone (4-NBTSc) using IR, 1HNMR and 13C NMR. The compound’s in vitro anticancer activities against different cell lines were evaluated. Molecular docking, Insilco ADMET, and drug-likeness prediction were also done. The test compounds showed a comparative IC50 and growth inhibition with the standard drug Doxorubicin. The IC50 ranges from 2.82 µg/mL to 14.25 µg/mL in 3-MBTSc and

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Bienvenu, GLINMA, KPADONOU Bénédicta, HAOUTHAOU Mirhane, F. AGNIMONHAN Hyacinthe, H. POUPAERT Jacques, and A. GBAGUIDI Fernand. "Cyclohexylphenylketone Thiosemicarbazones: Synthesis in the Green Chemistry Condition and Spectral Characterization." Journal of Scientific and Engineering Research 9, no. 12 (2022): 68–72. https://doi.org/10.5281/zenodo.10531905.

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<strong>Abstract</strong> Thiosemicarbazones and their derivatives have a significant awareness in the organic field, pharmacology, and biology; appreciations to their various applications. Their interest in medicinal chemistry has stimulated word researchers the development of new methods for their synthesis, respecting also the fundamental principles of green chemistry. In this paper, we reporte the synthesis of cyclohexylphenylketone thiosemicarbazone <strong>P<sub>1</sub></strong> and cyclohexylphenylketone 4-phenyl-3-thiosemicarbazone <strong>P<sub>2</sub></strong> with goods yields (81%

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Konstantinovic, Sandra, Milica Zlatkovic, Jovan Ciric, Slavica Ilic, Gordana Gojgic-Cvijovic, and Vlada Veljkovic. "The use of salicylaldehyde derivatives as a nitrogen source for antibiotic production by Streptomyces hygroscopicus CH-7." Chemical Industry 71, no. 6 (2017): 487–94. http://dx.doi.org/10.2298/hemind170124011k.

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In the present work, four derivatives of salicylaldehyde (salicylaldehyde-hydrazone, phenylhydrazone, semicarbazone and thiosemicarbazone) were synthesized using both conventional (95% ethanol) and green (crude glycerol from biodiesel production) solvents. The obtained compounds were identified by elemental microanalysis, as well as FTIR, UV/Vis and 1H-NMR spectroscopic methods. Yields of 93?98% of the compounds in crude glycerol were achieved within 10?25 min. The derivatives of salicylaldehyde and crude glycerol were used as a nitrogen and carbon source, respectively, in the medium for antib

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Sweidan, Kamal, Dima A. Sabbah, Sanaa Bardaweel, et al. "Facile synthesis, characterization, and cytotoxicity study of new 3-(indol-2-yl)bicyclotetrazatridecahexaens." Canadian Journal of Chemistry 95, no. 8 (2017): 858–62. http://dx.doi.org/10.1139/cjc-2017-0120.

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A new series of thiosemicarbazone-based indole derivatives 12–15 has been prepared by condensation reaction of indole-2-carboxamide derivatives 8–11 with thiosemicarbazide. The former compounds underwent intracyclization in the presence of chloroacetic acid and sodium acetate to afford a set of new 3-(indol-2-yl)bicyclotetrazatridecahexaens 16–19. These newly synthesized compounds have been characterized by means of FTIR, 1H NMR, 13C NMR, and HRMS and by elemental analyses. Cytotoxic activities of the prepared compounds along with LY294002 were evaluated in vitro against normal human skin fibr

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de Freitas, Beatriz C., Paula A. Queiroz, Vanessa P. Baldin, et al. "(-)-Camphene-based derivatives as potential antibacterial agents against Staphylococcus aureus and Enterococcus spp." Future Microbiology 15, no. 16 (2020): 1527–34. http://dx.doi.org/10.2217/fmb-2020-0131.

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Aim: To evaluate the activity of (-)-camphene-based thiosemicarbazide (TSC) and 4-hydroxy-thiosemicarbazone (4-OH-TSZ), alone and in combination against Gram-positive. Material & methods: MIC were determined for Staphylococcus aureus, Enterococcus spp. reference strains and clinical isolates. Drug combination, time–kill and cytotoxicity assays were also performed. Results: TSC and 4-OH-TSZ demonstrated potent inhibitory activity against S. aureus and Enterococcus spp., including multidrug-resistant isolates (MIC ranging from 1.9 to 31.2 μg/ml), and were bactericidal for the reference strai

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Bekier, Adrian, Anna Brzostek, Agata Paneth, et al. "4-Arylthiosemicarbazide Derivatives as Toxoplasmic Aromatic Amino Acid Hydroxylase Inhibitors and Anti-inflammatory Agents." International Journal of Molecular Sciences 23, no. 6 (2022): 3213. http://dx.doi.org/10.3390/ijms23063213.

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Approximately one-third of the human population is infected with the intracellular cosmopolitan protozoan Toxoplasma gondii (Tg), and a specific treatment for this parasite is still needed. Additionally, the increasing resistance of Tg to drugs has become a challenge for numerous research centers. The high selectivity of a compound toward the protozoan, along with low cytotoxicity toward the host cells, form the basis for further research, which aims at determining the molecular targets of the active compounds. Thiosemicarbazide derivatives are biologically active organic compounds. Previous s

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Aljuhani, Ateyatallah, Mohamed S. Nafie, Nader R. Albujuq, et al. "Discovery of new benzothiazole-1,2,3-triazole hybrid-based hydrazone/thiosemicarbazone derivatives as potent EGFR inhibitors with cytotoxicity against cancer." RSC Advances 15, no. 5 (2025): 3570–91. https://doi.org/10.1039/d4ra07540d.

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Gupta, Monika. "Synthesis and Anti Proliferative Activity of Thiosemicarbazone and 4-Thiazolidinones." International Journal of Pharmacognosy & Chinese Medicine 3, no. 3 (2019): 1–9. http://dx.doi.org/10.23880/ipcm-16000166.

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Thiosemicarbazone and 4-Thiazolidinones are heterocyclic compounds with a broad spectrum of biological activities such as anti-inflammatory, anti-viral, anti-bacterial, anti-fungal and anticancer. A series of ten derivatives of thiosemicarbazone and 4-thiazolidinones derivatives was synthesised and evaluated for their antiproliferative activity against human breast cancer cells (MCF-7). The structure of compounds was established by IR and 1HNMR spectral studies. The synthesized compounds possessed good to moderate anticancer activity using Adriamycin as a standard. Out of ten synthesized compo

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Saha, Dilip Kumar, Shreelekha Padhye, and Subhash Padhye. "Targeting Estrogen Receptor Sites in Human Breast Cancer Cell Line T47D With Copper Conjugates of Nonsteriodal Anti-inflammatory Drug Derivatives: Antiproliferative Activity of Ketoprofen Derivative and its Copper Complex." Metal-Based Drugs 8, no. 2 (2001): 73–77. http://dx.doi.org/10.1155/mbd.2001.73.

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A square planar copper complex of derivatized NSAID drug (Ketoprofen thiosemicarbazone [3-benzoyl-α -methyl benzene acetic acid thiosemicarbazone]), is characterized by elemental analysis, spectroscopy, electrochemistry and magnetic susceptibility studies which exhibits dose-dependent and enhanced antiproliferative effects on human breast cancer cell line T47D rich in progesterone receptors.

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Hu, Biao, Bo Wang, Bing Zhao, et al. "Thiosemicarbazone-based selective proliferation inactivators inhibit gastric cancer cell growth, invasion, and migration." MedChemComm 8, no. 12 (2017): 2173–80. http://dx.doi.org/10.1039/c7md00353f.

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Bahojb Noruzi, Ehsan, Behrouz Shaabani, Silvano Geremia, Neal Hickey, Patrizia Nitti, and Hossein Samadi Kafil. "Synthesis, Crystal Structure, and Biological Activity of a Multidentate Calix[4]arene Ligand Doubly Functionalized by 2-Hydroxybenzeledene-Thiosemicarbazone." Molecules 25, no. 2 (2020): 370. http://dx.doi.org/10.3390/molecules25020370.

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The design and synthesis of a novel tert-butyl-calix[4]arene functionalized at 1, 3 positions of the lower rim with two terminal 2-hydroxybenzeledene-thiosemicarbazone moieties is reported. The new ligand with multi-dentate chelating properties was fully characterized by several techniques: ESI-Mass spectroscopy, FT-IR, 1H-NMR, and single crystal X-ray diffraction. The solid state structure confirms that the calix[4]arene macrocycle has the expected open cone conformation, with two opposite phenyl rings inclined outwards with large angles. The conformation of the two alkoxythiosemicarbazone ar

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Khatun, Rabeya, AS Mansarul Islam, and MA Hai. "Synthesis of Schiff Base having a Heterocyclic Moiety along with its Cyclized Derivatives and Study of their Antifungal Activities." Journal of the Bangladesh Chemical Society 25, no. 1 (2012): 7–14. http://dx.doi.org/10.3329/jbcs.v25i1.11765.

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Syntheses of Schiffs base1 1-[(2, 4-difluorophenyl)-2-(1H-1, 2, 4-triazol-1-yl)] ethanone thiosemicarbazone (1A) prepared by condensation of 1-(2,4- difluorophenyl)-2-[1(H)-1,2,4-triazol-1-yl] ethanone with thiosemicarbazide, followed by cyclization2 to 2-(2,4-difluorophenyl)-2-[(1H)-1,2,4-triazol-1- ylmethyl)]-3-acetyl-5-acetylamino- thiadiazoline ( 2A), using acetic anhydride, and finally hydrolysis3 of (2A) to form 2-(2,4-difluorophenyl)-2-[(1H)-1,2,4-triazol-1- ylmethyl)]-3-acetyl-5-amino-thiadiazoline (3A), using hydrazine hydrate, all compounds having anti-fungal activities, are reporte

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Zhang, Honghong, Zhongnian Yang, Li Zhang, Wu Yue, Yanfeng Zhu, and Xian Zhang. "Inhibition performance of halogen-substituted benzaldehyde thiosemicarbazones as corrosion inhibitors for mild steel in hydrochloric acid solution." RSC Advances 12, no. 47 (2022): 30611–25. http://dx.doi.org/10.1039/d2ra05690a.

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Anand, Selvam Athavan Alias, Chandrasekaran Loganathan, Nisha Susan Thomas, Kuppusamy Saravanan, Antony Therasa Alphonsa, and Senthamaraikannan Kabilan. "Synthesis, structure prediction, pharmacokinetic properties, molecular docking and antitumor activities of some novel thiazinone derivatives." New Journal of Chemistry 39, no. 9 (2015): 7120–29. http://dx.doi.org/10.1039/c5nj01369k.

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Mendes, Goulart, Chaves, et al. "Evaluation of Novel Chalcone-Thiosemicarbazones Derivatives as Potential Anti-Leishmania amazonensis Agents and Its HSA Binding Studies." Biomolecules 9, no. 11 (2019): 643. http://dx.doi.org/10.3390/biom9110643.

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A series of seven chalcone-thiosemicarbazones (5a–5g) were synthesized and evaluated as potential new drugs (anti-leishmanial effect). Although four of the chalcone-thiosemicarbazones are already known, none of them or any compound in this class has been previously investigated for their effects on parasites of the Leishmania genus. The compounds were prepared in satisfactory yields (40–75%) and these compounds were evaluated against promastigotes, axenic amastigotes and intracellular amastigotes of L. amazonensis after 48 h of culture. The half maximal inhibitory concentration (IC50) values o

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Garcia Santos, Isabel, Adelheid Hagenbach, and Ulrich Abram. "Stable gold(iii) complexes with thiosemicarbazone derivatives." Dalton Trans., no. 4 (2004): 677–82. http://dx.doi.org/10.1039/b312978k.

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Adhikari, Hari Sharan. "Enhancement in Anticancer Activity of Chitosan Tailored Imidazole-2-Thiosemicarbazones against MCF-7 Cancer Cell Line by Coordination with Copper(II) Ions." Journal of Engineering and Sciences 3, no. 1 (2024): 1–8. http://dx.doi.org/10.3126/jes2.v3i1.66226.

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The coordination behavior of new batch synthesized chitosan imidazole-2-thiosemicarbazones tailored from both the low molecular weight commercial chitosan and high molecular weight crab shell chitosan was confirmed by Fourier Transform Infrared (FT-IR) and magnetic susceptibility measurements. Chlorine content in the complexes was estimated by potentiometric titration technique. The study showed the tridentate NNS tridentate coordination with copper (II) ion in a square planar orientation with the remaining valence satisfied by coordination with chloride ion. The MTT assay studies showed an en

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Peretz, Eliav, Noa Ashkenazi, and Sanaa Musa. "Cannabidiol-Based Thiosemicarbazones: A Preliminary Study Evaluating Their Anti-Tyrosinase Properties." Molecules 30, no. 6 (2025): 1291. https://doi.org/10.3390/molecules30061291.

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Cannabidiol (CBD), a non-psychoactive cannabinoid, has attracted significant research interest due to its antioxidant, anti-inflammatory, and neuroprotective properties. As a versatile scaffold in drug discovery, CBD has been widely explored for developing novel therapeutics. In this study, we synthesized and evaluated the anti-tyrosinase activity of CBD-based thiosemicarbazones. Structure–activity relationship (SAR) analyses were conducted to assess the impact of various functional groups on tyrosinase inhibition, including an evaluation of inhibitory kinetics for selected compounds. The synt

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