二芳基取代-1,2,4-三唑类化合物的合成及其抗炎活性研究  

Synthesis and Anti-inflammatory Activities of Diaryl-substituted-1,2,4-trizole Derivatives

作　　者：徐进宜[1] 姚和权[1] 曾翼[1] 华维一[1] 吴晓明[1] 王秋娟[2] 胡松[2] 吴雪丰[2] 岳攀[2] 

机构地区：[1]中国药科大学药物化学教研室 [2]中国药科大学生理学教研室,南京210009

出　　处：《高等学校化学学报》2005年第12期2254-2258,共5页Chemical Journal of Chinese Universities

基　　金：教育部优秀青年教师基金(批准号:2003355);江苏省自然科学基金(批准号:BK2004109)资助

摘　　要：以选择性环氧化酶-2(COX-2)抑制剂Celecoxib为先导,根据其构效关系和分子模拟研究结果,应用生物电子等排原理等药物设计方法,设计合成了19个结构全新的二芳基取代-1,2,4-三唑类衍生物,其结构经IR,1H NMR,MS和元素分析确证.初步的药理试验结果表明,部分目标化合物具有一定的抗炎活性.Nonsteroidal anti-inflammatory durgs（NSAIDs） are among the most widely prescribed medications with their uses limited by significant toxicity. The studies of the cyclooxygenase （COX） show that the side effects of classical NSAIDs come from the inhibition of COX-1, while the therapeutic effects come from the inhibition of COX-2. Selective COX-2 inhibitors were developed as NSAIDs which display the profiles of good potent activities and low side effects. In order to search for the new NSAIDs, using the marketed selective COX-2 inhibitor celecoxib as a leading compound and based on the result of molecular modeling study of COX- 2 inhibitors, a series of novel diaryl-substituted-1,2,4-trizole derivatives were designed and synthesized. All the target compounds were confirmed by IR, MS, ^1H NMR spectra and elemental analysis. The results of preliminary pharmacological tests in vivo show that some compounds have certain anti-inflammatory effect.

关 键 词：1 2 4-三唑类衍生物 合成 选择性环氧化酶-2抑制剂 抗炎 

分 类 号：O626[理学—有机化学]