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

被引：3

作者：

Liu, Xuefei ^{[1
]}

Chen, Qianqian ^{[1
]}

Zhu, Ju ^{[1
]}

Fan, Yongzheng ^{[1
]}

Ding, Lili ^{[1
]}

Zhao, Juntao ^{[1
]}

Han, Guangqian ^{[2
]}

Tian, Wei ^{[1
]}

Qi, Jingjing ^{[1
]}

Zhou, Youjun ^{[1
]}

Lv, Jiaguo ^{[1
]}

机构：

[1] Second Mil Med Univ, Dept Med Chem, Sch Pharm, Shanghai 200433, Peoples R China

[2] Fujian Agr & Forestry Univ, Dept Pharmacognosy, Sch Food Sci, Fuzhou 350002, Fujian, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 10期

关键词：

acrosin inhibitory agents; synthesis; methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamate; ORAL-CONTRACEPTIVE PILL; HUMAN-SPERMATOZOA; SPERM; SEMEN;

D O I：

10.1016/j.bmcl.2012.03.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 IC50 of 6.3 x 10 (5) M. The studies provide a new structural class for the development of novel acrosin inhibitory agents. Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.

引用

页码：3554 / 3559

页数：6

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