期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 14, 页码 4177-4184出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.031
关键词
Acrosin inhibitory activity; Synthesize; 5-Phenyl-1H-pyrazole-3-carboxylic acid amide
资金
- Science and Technology, Jiang Su [BE2010682]
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. CompoundsAQ-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 0.01 mu mol/mL. This study provided a new structural class for the development of novel acrosin inhibitory agents. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.
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