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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu X,Chen Q,Zhu J,Fan Y,Ding L,Zhao J,Han G,Tian W,Qi J,Zhou Y,Lv J

doi

10.1016/j.bmcl.2012.03.042

subject

Has Abstract

pub_date

2012-05-15 00:00:00

pages

3554-9

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00363-0

journal_volume

22

pub_type

杂志文章

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