| 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 |
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| 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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| 作者姓名： | 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 |
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| 作者单位： | 第二军医大学药学院药物化学教研室,上海,200433 |
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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3g是对照物Na-对甲苯磺酰-L-赖氨酸氯甲基酮（TLCK）的229倍。
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| 关 键 词： | 精子顶体酶 抑制剂 设计 合成 抑酶 喹唑啉酮 |
| 收稿时间： | 2010/1/19 0:00:00 |
| 修稿时间： | 3/9/2010 12:00:00 AM |
Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor |
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| NING Wei-wei,LIU Xue-fei,ZHANG Xiao-meng,ZHENG Can-hui,SHENG Chun-quan,ZHOU You-jun,ZHANG Ling,LV Jia-guo and ZHU Ju.Design,synthesis of novel quinazolinon compounds as human anti-acrosin inhibitor[J].The Journal of Pharmaceutical Practice,2010,28(4):296-298,312. |
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| Authors: | NING Wei-wei LIU Xue-fei ZHANG Xiao-meng ZHENG Can-hui SHENG Chun-quan ZHOU You-jun ZHANG Ling LV Jia-guo and ZHU Ju |
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| Institution: | Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China;Department of Medicinal Chemistry,School of Pharmacy,Second Military Medical University,Shanghai 200433,China |
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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. |
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| Keywords: | acrosin inhibitor design synthesis anti-acrosin activity quinazolinon |
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