Synthesis and Structure-Activity Relationship of Thioacetamide-Triazoles against Escherichia coli.

ABSTRACT: Infections due to Gram-negative bacteria are increasingly dangerous due to the spread of multi-drug resistant strains, emphasizing the urgent need for new antibiotics with alternative modes of action. We have previously identified a novel class of antibacterial agents, thioacetamide-triazoles, using an antifolate targeted screen and determined their mode of action which is dependent on activation by cysteine synthase A. Herein, we report a detailed examination of the anti-E. coli structure-activity relationship of the thioacetamide-triazoles. Analogs of the initial hit compounds were synthesized to study the contribution of the aryl, thioacetamide, and triazole sections. A clear structure-activity relationship was observed generating compounds with excellent inhibition values. Subst

SUBMITTER: Dharuman S 

PROVIDER: S-EPMC8911640 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature