Microbial infection remains a global health threat and there is a continuous rise in associated mortality rates. The current study reports the resynthesis of thirteen thiazolyl-2-chloroacetamide derivatives (4a-4m) by using optimization of base, solvent and their molar equivalent ratio to improve yield and such thiazole derivatives as potential antimicrobial agents. We present the resynthesis data and confirm the compound structures using spectroscopic techniques. The compounds were evaluated for antimicrobial potential using standard methods. The antimicrobial activity of all the compounds were compared to the standard drug erythromycin against Bacillus subtilis, azithromycin against Escherichia coli, and fluconazole against Aspergillus niger. The compounds 4a, 4f, 4g, and 4j showed the best MIC value against Gram-positive bacteria (B. subtilis), compounds 4f and 4j with the best MIC value against Gram-negative bacteria (E. coli), and 4c, 4g, 4j, and 4k with the best MIC value against fungal species (A. niger). Particularly, the compounds 4j and 4f showed the best MIC values against all stains. Also, molecular docking studies revealed that the docking calculations and the experimental data are in close proximate.
Keywords: antimicrobial activity; synthesis optimization; thiazolyl‐2‐chloroacetamide.
© 2025 Wiley‐VHCA AG, Zurich, Switzerland.