新型喹唑啉酮类先导物的设计、合成及抑制人顶体酶活性研究  

Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor

作　　者：宁微微[1] 刘雪飞[1] 张晓梦[1] 郑灿辉[1] 盛春泉[1] 周有骏[1] 章玲[1] 吕加国[1] 朱驹[1] 

机构地区：[1]第二军医大学药学院药物化学教研室,上海200433

出　　处：《药学实践杂志》2010年第4期296-298,312,共4页Journal of Pharmaceutical Practice

摘　　要：目的基于人精子顶体酶活性位点的三维结构设计并合成新型3-取代喹唑啉酮类化合物。方法计算机模拟设计及化学合成。结果设计并合成了7个3-取代喹唑啉酮类先导物,进行了抑酶活性测试。结论所有合成的化合物具有较好的抑酶活性,其中化合物3 g是对照物Nα-对甲苯磺酰-L-赖氨酸氯甲基酮(TLCK)的229倍。Objective Novel 3-substituted quinazolinon compounds were designed and synthesised on the base of the active site of human acrosin. Methods The compounds were designed by computer and chemically synthesised. Results Seven 3-substituted quinazolinon compounds were designed and synthesised,subsequently carried out in vitro anti-acrosin test. Conclusion The results of anti-acrosin tese in vitro exhibited that all the compounds showed potent anti-acrosin activities. Particularly, compounds 3 g displayed much stronger anti-acrosin activities（229 times） than that of TLCK.

关 键 词：精子顶体酶 抑制剂 设计 合成 抑酶 喹唑啉酮 

分 类 号：R914[医药卫生—药物化学]