5-苯基-1H-吡唑-3-羧酸酰胺衍生物的合成及其顶体酶抑制活性。
Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives.
机构信息
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
出版信息
Bioorg Med Chem Lett. 2013 Jul 15;23(14):4177-84. doi: 10.1016/j.bmcl.2013.05.031. Epub 2013 May 22.
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.
设计、合成了一系列新型 5-苯基-1H-吡唑-3-羧酸酰胺衍生物，并对其体外的顶体蛋白酶抑制活性进行了评价。顶体蛋白酶抑制活性结果表明，所有目标化合物均比对照 TLCK 具有更强的活性。化合物 AQ-A1、AQ-D3、AQ-D4、AQ-E4 和 AQ-E5 的顶体蛋白酶抑制活性均强于对照 ISO-1。特别是化合物 AQ-E5 在所有化合物中表现出最强的顶体蛋白酶抑制活性，IC50 为 0.01μmol/mL。本研究为开发新型顶体蛋白酶抑制剂提供了一个新的结构类型。
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