Rational design and synthesis of novel phenyltriazole derivatives targeting MRSA cell wall biosynthesis.

ABSTRACT: Antimicrobial resistance in methicillin-resistant Staphylococcus aureus (MRSA) is a major global health challenge. This study reports the design and synthesis of novel phenyltriazole derivatives as potential anti-MRSA agents. The new scaffold replaces the thiazole core with a 1,2,3-triazole ring, enhancing antimicrobial efficacy and physicochemical properties. A series of derivatives were synthesized and evaluated, with four compounds (20, 23, 29 and 30) showing significant activity against MRSA (MIC ≤ 4 μg mL^-1). Compound 29 emerged as the most promising candidate, showing rapid bactericidal activity and superior performance over vancomycin in time-kill assays. It exhibited selective toxicity against bacterial cells, minimal cytotoxicity in human cell lines and low hemol

SUBMITTER: Elsebaei MM 

PROVIDER: S-EPMC11659749 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature