Background: Antimicrobial resistance is a major global health problem, which is being
rapidly deteriorating the quality of human health. Series of substituted N-(benzo[d]thiazol-2-yl)-2-
(4-(6-fluorobenzo[d]isoxazol-3-yl) piperidin-1-yl)acetamide (3a-j) were synthesized from substituted
N-(benzo[d]thiazol-2-yl)-2-chloroacetamide/bromopropanamide (2a-j) and 6-fluoro-3-
(piperidin-4-yl)benzo[d]isoxazole (2) and further evaluated for their docking properties and antimicrobial
Methods: All the synthesized compounds were characterized by FT-IR, NMR and Mass spectral
analysis. All compounds were allowed to dock against different antimicrobial targets having PDB
ID: 1D7U and against common antifungal target having PDB ID: 1EA1.
Results: The compounds 3d and 3h showed good activity against Methicillin-resistant Staphylococcus
aureus (MRSA, resistance Gram-positive bacteria). All synthesized compounds showed
good to moderate activity against selected bacterial and fungal microbial strains. If we compared
the actual in-vitro antimicrobial activity and in silico molecular docking study, we found that molecules
3i and 3h were more potent than the others.
Conclusion: Our current study would definitely pave the new way of designing and synthesis of
more potent 2-aminobenzothiazoles derivatives.