| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591504 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
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 the control TLCK. Of all compounds, compound AQ-E5 displayed the most potent acrosin inhibitory activity, with an IC50 of 0.01 μmol/mL and the docking result of compound AQ-E5 within the active site of acrosin was as follows.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wei Tian, Guangqian Han, Ju Zhu, Jingjing Qi, Qianqian Chen, Juntao Zhao, Canhui Zheng, Ling Zhang, Youjun Zhou, Jiaguo Lv,