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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Letter Article

Synthesis and Antimicrobial Activity of Functional Derivatives of thiazolo[ 2,3-c][1,2,4]triazoles

Author(s): Mikhailo Slivka*, Maksym Fizer, Ruslan Mariychuk, Marek Ostafin, Olexander Moyzesh, Galyna Koval, Oksana Holovko-Kamoshenkova, Ivan Rusyn and Vasyl Lendel

Volume 19, Issue 9, 2022

Published on: 01 February, 2022

Page: [791 - 799] Pages: 9

DOI: 10.2174/1570180819666220110145659

Price: $65

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Abstract

Background: Condensed triazoles are a well-known class of heterocyclic compounds due to a wide range of biological activities. The study is dedicated to the evaluation of the antimicrobial potential of new functional derivatives of thiazolo[2,3-c][1,2,4]triazoles.

Methods: Effective, easy-to-implement and low-cost routes for production of title compounds via electrophilic intramolecular heterocyclization are reported. Bactericidal and fungicidal activities against Gram-positive and Gram-negative bacteria and fungus were studied. The influence of functional groups on the biological activity of tested thiazolo[2,3-c][1,2,4]triazoles is discussed.

Results: Microbiological evaluation shows that 6-[(trichlorotellanyl)methyl]-[1,3]thiazolo[2,3- c][1,2,4]triazol-3-amine hydrogen chloride 2a and 3-(2-hydroxyphenyl)-6-[(trichloro-λ4-tellanyl)methyl]- 5,6-dihydro-[1,3]thiazolo[2,3-c][1,2,4]triazole 2g have a high bactericidal activity and Cu (I) salts of 3-(2- hydroxyphenyl)-6-iodomethyl/6-methylidene-5,6-dihydro-[1,3]thiazolo-[2,3-c][1,2,4]triazoles 5a,c have a high fungicidal activity.

Conclusion: It is concluded that these products or their derivatives may be of practical benefit as bactericidal and fungicidal agents.

Keywords: Thiazolo[2, 3-c][1, 2, 4]triazole, electrophilic heterocyclization, tellurium tetrachloride, tellurium tetrabromide, copper salt, fungicidal and bactericidal activities.

Graphical Abstract
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