| 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 |
| 投稿时间：2010-01-19 修订日期：2010-03-09 点此下载全文 |
| 引用本文：宁微微,刘雪飞,张晓梦,郑灿辉,盛春泉,周有骏,章玲,吕加国,朱驹.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[J].药学实践杂志,2010,28(4):296~298,312 |
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| 中文摘要: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。 |
| 中文关键词:精子顶体酶 抑制剂 设计 合成 抑酶 喹唑啉酮 |
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| Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor |
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| Abstract:ObjectiveNovel 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. |
| keywords:acrosin inhibitor design synthesis anti-acrosin activity quinazolinon |
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