1338234-75-5Relevant academic research and scientific papers
Discovery of novel guanidinophenylpyrazole human acrosin inhibitors by molecular hybridization
Zhao, Juntao,Sun, Nannan,Gao, Yue,Lv, Diya,Liu, Yang,Jiang, Yan,Dong, Guoqiang,Chen, Qianqian,Li, Wei,Zhou, Youjun,Zhu, Ju,Sheng, Chunquan,Lv, Jiaguo
, p. 1520 - 1527 (2014)
Human acrosin is a promising target for male contraceptives. A series of novel guanidinophenylpyrazole derivatives were rationally designed by molecular hybridization of the phenylpyrazole and guanidinobenzoate inhibitors. Most of the target compounds showed potent human acrosin inhibitory activities. In particular, compound F3 was a highly active human acrosin inhibitor (IC50 = 1.26 μM) with good selectivity over trypsin. Molecular docking studies revealed that compound F3 formed hydrophobic and hydrogen bonding interactions with the active site of human acrosin. Compound F3 represents a promising lead compound for the development of novel male contraceptives.
Pyrromonazole acrosomal enzyme inhibitor and method for preparing same
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, (2016/11/17)
The invention relates to a novel acrosin inhibitor, a preparation method and application in preparation of male antifertility drugs thereof. Specifically, the invention relates to a novel acrosin inhibitor shown as formula I, wherein all substituents are defined as the specification. The invention also relates to the preparation method of the acrosin inhibitor and application in preparation of male antifertility drugs. (formula I).
Synthesis and acrosin inhibitory activities of substituted ethyl 5-(4-aminophenyl)-1H-pyrazole-3-carboxylate derivatives
Qi, Jingjing,Zhu, Ju,Liu, Xuefei,Ding, Lili,Zheng, Canhui,Han, Guangqian,Lv, Jiaguo,Zhou, Youjun
, p. 5822 - 5825 (2011/10/18)
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.
