New Benzamide Analogues of Metronidazole-tethered Triazoles as Non-sugar Based Inhibitors of β-Glucuronidase

摘要

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 differ- ent 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.