Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
Bioorg Med Chem Lett. 2011 Oct 1;21(19):5822-5. doi: 10.1016/j.bmcl.2011.07.110. Epub 2011 Aug 3.
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.
设计合成了一系列新型的 5-(4-氨基苯基)-1H-吡唑-3-羧酸乙酯衍生物，并对其体外弹性蛋白酶抑制活性进行了评价。大多数化合物表现出弹性蛋白酶抑制活性。其中，三个化合物（5l、5n 和 5v）比对照 TLCK 更有效。这些为开发新型避孕弹性蛋白酶抑制剂提供了新的结构类型。
