title: Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives.
abstract: A series of novel methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamates were designed, synthesized, and their acrosin inhibitory activities evaluated in vitro. The results of acrosin inhibitory activity showed that all title compounds were more potent than the control TLCK. Compound 4w displayed the most potent acrosin inhibitory activity among all the compounds, with an IC(50) of 6.3×10(-5)M. The studies provide a new structural class for the development of novel acrosin inhibitory agents.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Xuefei
authors.initials: X
authors.lastname: Liu
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Chen
authors.forename: Ju
authors.initials: J
authors.lastname: Zhu
authors.forename: Yongzheng
authors.initials: Y
authors.lastname: Fan
authors.forename: Lili
authors.initials: L
authors.lastname: Ding
authors.forename: Juntao
authors.initials: J
authors.lastname: Zhao
authors.forename: Guangqian
authors.initials: G
authors.lastname: Han
authors.forename: Wei
authors.initials: W
authors.lastname: Tian
authors.forename: Jingjing
authors.initials: J
authors.lastname: Qi
authors.forename: Youjun
authors.initials: Y
authors.lastname: Zhou
authors.forename: Jiaguo
authors.initials: J
authors.lastname: Lv
mesh_terms: D000176:Acrosin / Q000037:antagonists & inhibitors*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008958:Models, Molecular
chemical_list: D001562:Benzimidazoles; D000176:Acrosin