The present study describes the synthesis, and evaluation of β‐glucuronidase inhibitory potential of metronidazole analogues. Twenty‐four metronidazole‐tethered benzamide triazoles (28‐51) were synthesized using copper‐catalyzed Huisgen alkyne‐azide cycloaddition reaction, and characterized by using different spectroscopic techniques. All of them were identified as new compounds. Compounds 28–51 demonstrated weak to excellent in vitro β‐glucuronidase inhibitory activity with no toxicity against 3T3 mouse fibroblast cell lines. Compound 51 (IC50=12.41 ± 0.58 μM) was found to be the most active β‐glucuronidase inhibitor among the series, with an activity ∼4 times higher than the standard inhibitor, D‐saccharic acid‐1,4‐lactone (IC50=45.75 ± 2.16 μM).