title: Synthesis and β-glucuronidase inhibitory potential of benzimidazole derivatives.
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.
authors.affiliation: H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. hassaan2@super.net.pk
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
authors.forename: Momin
authors.initials: M
authors.lastname: Khan
authors.forename: Nida
authors.initials: N
authors.lastname: Ambreen
authors.forename: Fazal
authors.initials: F
authors.lastname: Rahim
authors.forename: Shagufta
authors.initials: S
authors.lastname: Naureen
authors.forename: Shahnaz
authors.initials: S
authors.lastname: Perveen
authors.forename: M Iqbal
authors.initials: MI
authors.lastname: Choudhary
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Voelter
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005966:Glucuronidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008099:Liver / Q000201:enzymology; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D004791:Enzyme Inhibitors; C031000:benzimidazole; D005966:Glucuronidase