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Synthesis and β-Glucuronidase Inhibitory Potential of Benzimidazole Derivatives

[ Vol. 8 , Issue. 3 ]

Author(s):

Khalid Mohammed Khan, Momin Khan, Nida Ambreen, Fazal Rahim, Shagufta Naureen, Shahnaz Perveen, M. Iqbal Choudhary and Wolfgang Voelter   Pages 421 - 427 ( 7 )

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.

Keywords:

Benzimidazole, β-glucuronidase inhibition, glucuronosyl-O-bonds, antihelmintic, anticoagulant, leukaemia, antihistaminic, antihypertensive, dimethylformamide, lepromatous

Affiliation:

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.



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