Synthesis and β-glucuronidase inhibitory potential of benzimidazole derivatives
Khalid Mohammed Khan1, Momin Khan, Nida Ambreen
1H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. hassaan2@super.net.pk
Abstract:
Benzimidazole derivatives 1-24 have been synthesized and their in vitro β-glucuronidase inhibitory activitiy was evaluated. Compounds 15 (IC50=6.33+/-0.40 μM), 7 (IC50=22.0+/-0.33 μM), 2 (IC50=23.1+/-1.78 μM), 17 (IC50=23.9+/-1.46 μM), and 3 (IC50=33.8+/-1.61 μM) showed more potent β-glucuronidase inhibitory activity than the standard (D-saccharic acid 1,4 lactone, IC50=48.4+/-1.25 μM). This study has identified a new series of potential β-glucuronidase inhibitors. A structure-activity relationship has also been studied.
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