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
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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。Abstract: 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.
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Key words:
- acrosin inhibitor /
- design /
- synthesis /
- anti-acrosin activity /
- quinazolinon /
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