Design, Synthesis, and Biological Evaluation of 1,2,4-Triazole Derivatives as Potential Antimicrobial Agents

Authors : Yıldız UYGUN CEBECI

Pages : 69-77

Doi:10.34088/kojose.1060112

View : 51 | Download : 86

Publication Date : 2023-05-31

Article Type : Research Paper

Abstract :In this study, we aimed to develop new biologically active compounds with antibacterial properties. 4-amino-5-methyl-2H-1,2,4-triazol-3insert ignore into journalissuearticles values(4H);-one insert ignore into journalissuearticles values(1); was converted to the corresponding Schiff bases insert ignore into journalissuearticles values(2); with the reaction with a 4-anis aldehyde. Acetic acid ethyl esters containing [1,2,4] triazole ring insert ignore into journalissuearticles values(3); were synthesized by the condensation of compounds insert ignore into journalissuearticles values(2); with ethyl bromoacetate in basic media. The reaction of compounds insert ignore into journalissuearticles values(3); with hydrazine hydrate led to the formation of acid hydrazides insert ignore into journalissuearticles values(4);. The reaction of hydrazide insert ignore into journalissuearticles values(4); with phenyl isothio - and phenyl isocyanate produced the corresponding carbothioamide insert ignore into journalissuearticles values(5a); and carboxamide insert ignore into journalissuearticles values(5b);. The basic treatment of carbothioamide insert ignore into journalissuearticles values(5a); and. carboxamide insert ignore into journalissuearticles values(5b); produced 1,2,4-triazole insert ignore into journalissuearticles values(6a, 6b); compounds, respectively. The reactions of insert ignore into journalissuearticles values( insert ignore into journalissuearticles values(6b); with norfloxacin and ciprofloxacin in the presence of formaldehyde afforded the corresponding Mannich basesinsert ignore into journalissuearticles values( 7a, 7b);. The structural assignments of the new compounds were based on elemental analysis and spectral insert ignore into journalissuearticles values(IR, 1H-NMR, and 13C-NMR); data. All newly synthesized compounds were screened for their antimicrobial activity. The in vitro antimicrobial activities of the compounds were evaluated against pathogenic microorganisms, and compounds 7a and 7b were found the most effective antimicrobial activity.
Keywords : 1, 2, 4 triazole, fluoroquinolone, antimicrobial activity, multicomponent