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Letters in Drug Design & Discovery

Editor-in-Chief

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

Research Article

Synthesis, Antibacterial, Antifungal, Antimycobacterial Activity Evaluation of Novel 1,2,4-triazole Derivatives Bearing 4-Aminophenyl Moiety

Author(s): Betul Kaya Cavusoglu, Leyla Yurttas, Meral Y. Cankilic and Zafer A. Kaplancikli

Volume 14, Issue 8, 2017

Page: [938 - 948] Pages: 11

DOI: 10.2174/1570180814666161130103624

Price: $65

Abstract

Background: In this work, 2-[[5-(4-aminophenyl)-4-(4-substituted phenyl)-4H-1,2,4- triazol-3-yl]thio]-1-(4-substituted phenyl)ethan-1-one derivatives (1-15) and 2-[[5-(4-aminophenyl)- 4-(4-substituted phenyl)-4H-1,2,4-triazol-3-yl]thio]-N-(4-substituted phenyl)acetamide derivatives (15-30) were synthesized using 4-aminobenzohydrazide as starting material.

Methods: These compounds were screened to determine their antimicrobial activities against Grampositive bacteria B. cereus, S. aureus, E. faecalis, L. monocytogenes; Gram-negative bacteria E. coli, P. aeruginosa, K. pneumoniae, S. typhimurium, yeasts C. parapsilosis, C. albicans, C. glabrata, C. krusei; molds A. niger, A. flavus, A. parasiticus, A. fumigatus, Rhizopus sp., A. alternate, S. rolfsii and a mycobacteria M. tuberculosis.

Results and Conclusion: Compounds 2, 6, 7, 8 have displayed antituberculotic potential as much as standard drug, rifampicin. Also, compounds have exhibited moderate antibacterial and antifungal activities, contrary to expectations.

Keywords: 1, 2, 4-Triazole, antibacterial, antifungal, antimycobacterial, tuberculosis (TB), multidrug resistant (MDR).

Graphical Abstract

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