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Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives. 2011
Jingjing Qi, and
Ju Zhu, and
Xuefei Liu, and
Lili Ding, and
Canhui Zheng, and
Guangqian Han, and
Jiaguo Lv, and
Youjun Zhou
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
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.
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