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Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives
Authors:Qi Jingjing  Zhu Ju  Liu Xuefei  Ding Lili  Zheng Canhui  Han Guangqian  Lv Jiaguo  Zhou Youjun
Institution:Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
Abstract:A series of novel ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives were designed and synthesized and their in vitro acrosin inhibitory activities were evaluated. Most of the compounds exhibited acrosin inhibitory activities. Among them, three compounds (5l, 5n, and 5v) were more potent than that of the control TLCK. These provide a new structural type for the development of novel contraceptive acrosin inhibitory agents.
Keywords:Acrosin inhibitory agents  Synthesis  Ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate
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