Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives

Xuefei Liu; Qianqian Chen; Ju Zhu; Yongzheng Fan; Lili Ding; Juntao Zhao; Guangqian Han; Wei Tian; Jingjing Qi; Youjun Zhou; Jiaguo Lv

doi:10.1016/j.bmcl.2012.03.042

Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives

Bioorg Med Chem Lett. 2012 May 15;22(10):3554-9. doi: 10.1016/j.bmcl.2012.03.042. Epub 2012 Mar 21.

Authors

Xuefei Liu¹, Qianqian Chen, Ju Zhu, Yongzheng Fan, Lili Ding, Juntao Zhao, Guangqian Han, Wei Tian, Jingjing Qi, Youjun Zhou, Jiaguo Lv

Affiliation

¹ Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.

PMID: 22507960
DOI: 10.1016/j.bmcl.2012.03.042

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Acrosin / antagonists & inhibitors*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology*
Magnetic Resonance Spectroscopy
Mass Spectrometry
Models, Molecular

Substances

Benzimidazoles
Acrosin