| Literature DB >> 23746472 |
Wei Tian1, Guangqian Han, Ju Zhu, Jingjing Qi, Qianqian Chen, Juntao Zhao, Canhui Zheng, Ling Zhang, Youjun Zhou, Jiaguo Lv.
Abstract
A series of novel 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives were designed, synthesized, and their acrosin inhibitory activities in vitro were evaluated. The results of the acrosin inhibitory activity showed that all target compounds were more potent than control TLCK. Compounds AQ-A1, AQ-D3, AQ-D4, AQ-E4 and AQ-E5 exhibited stronger acrosin inhibitory activities than control ISO-1. Especially, compound AQ-E5 displayed the most potent acrosin inhibitory activity in all the compounds, with an IC50 of 0.01μmol/mL. This study provided a new structural class for the development of novel acrosin inhibitory agents. CrownEntities:
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Year: 2013 PMID： 23746472 DOI： 10.1016/j.bmcl.2013.05.031
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823