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  

Design, Synthesis and in vitro Evaluation of Thiazole Derivatives of Naproxen as Cyclooxygenase-2 Inhibitors

作　　者：郭长彬[1,2] 郭彦伸[1] 郭宗儒[1] 肖景发[1] 褚凤鸣[1] 程桂芳[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050 [2]现在军事医学科学院毒物药物研究所从事博士后研究工作.

出　　处：《化学学报》2006年第15期1559-1564,共6页Acta Chimica Sinica

基　　金：国家自然科学基金(No.20072057)资助项目.

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.Based on the differences between cyclooxygenase-2 （COX-2） and COX-l, 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.

关 键 词：萘普生 环氧合酶-2 抑制剂 噻唑衍生物 

分 类 号：R914[医药卫生—药物化学]