| 萘普生噻唑衍生物的设计和合成及其环氧合酶-2抑制活性的体外评价 |
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| 引用本文： | 郭长彬,郭彦伸,郭宗儒,肖景发,褚凤鸣,程桂芳.萘普生噻唑衍生物的设计和合成及其环氧合酶-2抑制活性的体外评价[J].化学学报,2006,64(15):1559-1564. |
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| 作者姓名： | 郭长彬 郭彦伸 郭宗儒 肖景发 褚凤鸣 程桂芳 |
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| 作者单位： | 1. 军事医学科学院毒物药物研究所
2. 中国医学科学院中国协和医科大学药物研究所,北京,100050 |
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| 摘 要： | 基于环氧合酶-2 (COX-2)与COX-1结构上的差异, 设计了萘普生的噻唑衍生物, 以期利用COX-2的侧面口袋, 增加对COX-2的结合作用. 以萘普生为原料经四步反应合成7个目标化合物, 其结构经核磁共振氢谱、质谱和元素分析(或高分辨质谱)确证. 体外筛选结果表明, 化合物有一定的COX-2抑制活性.
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| 关 键 词： | 萘普生 环氧合酶-2 抑制剂 噻唑衍生物 |
| 收稿时间： | 10 24 2005 12:00AM |
| 修稿时间： | 2005-10-242006-04-24 |
Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors |
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| GUO,Chang-Bin,GUO,Yan-Shen,GUO,Zong-Ru,XIAO,Jing-Fa,CHU,Feng-Ming,CHENG,Gui-Fang.Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors[J].Acta Chimica Sinica,2006,64(15):1559-1564. |
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| Authors: | GUO Chang-Bin GUO Yan-Shen GUO Zong-Ru XIAO Jing-Fa CHU Feng-Ming CHENG Gui-Fang |
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| Institution: | Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050 |
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| Abstract: | Based on the differences between cyclooxygenase-2 (COX-2) and COX-1, a series of derivatives of naproxen in which the carboxyl group was replaced with a variety of substituted thiazolyls were designed. Seven target compounds were synthesized in four steps with naproxen as a starting material and structurally confirmed by 1H NMR, MS and elemental analysis or HRMS. The biological tests showed that some of them have inhibitory activity against COX-2 in vitro. |
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| Keywords: | naproxen cyclooxygenase-2 inhibitor thiazole derivative |
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