Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives

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• 作者：Wei Tian ; Guangqian Han ; Ju Zhu ; Jingjing Qi ; Qianqian Chen ; Juntao Zhao ; Canhui Zheng ; Ling Zhang ; Youjun Zhou ; Jiaguo Lv
• 关键词：Acrosin inhibitory activity ; Synthesize ; 5-Phenyl-1H-pyrazole-3-carboxylic acid amide
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：15 July, 2013
• 年：2013
• 卷：23
• 期：14
• 页码：4177-4184
• 全文大小：2303 K

文摘

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 0.01 ¦Ìmol/mL. This study provided a new structural class for the development of novel acrosin inhibitory agents.