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.