A series of novel N‐((l‐benzyl‐lH‐l,2,3‐triazol‐5‐yl) methyl)‐4‐(6‐methoxy benzo[d]thiazol‐2‐yl)‐2‐nitrobenzamide derivatives were prepared from 4‐(6‐methoxybenzo[d]thiazol‐2‐yl)‐2‐nitro‐N‐(prop‐2‐ynyl) benzamide with benzyl azides by using click reaction (copper‐catalyzed Huisgen 1,3‐dipolar cycloaddition reaction) in the presence of CuSO4.5H2O and sodium ascaorbate. All the newly synthesized compounds were evaluated further in vitro antimicrobial activity against Gram‐positive bacteria (Staphylococcus aureus and Bacillus subtillis), Gram‐negative bacteria (Echerichia coli and Pseudomonas aeuroginosa), and fungi (Aspergillus niger and Aspergillusfumigatus) strains. The new compounds were characterized based on spectroscopic evidence. Among them compounds 10a, 10h, and 10i were showed promising activity when compared with standard drugs Ciprofloxacin and Miconazole.