替米沙坦及其类似物的合成和生物活性研究

设计合成了替米沙坦及其类似物, 改进了替米沙坦的合成工艺. 用邻苯二胺与相应的有机羧酸缩合, 所得产物苯并咪唑衍生物与4'-溴甲基联苯-2-甲酸甲酯通过N-烷基化得到相应的目标化合物, 合成了替米沙坦和9种未见文献报道的苯并咪唑联苯化合物, 其结构经¹H NMR, IR, MS和元素分析确证. 用体外动脉环的方法, 研究目标化合物的初步体外抗高血压活性, 试验结果表明其中部分化合物具有一定的抗高血压活性.

Synthesis of Telmisartan and Its Derivatives and Evaluation of Their Biological Activities

The synthetic route of telmisartan and its derivatives was developed and improved. The conden- sation of o-phenylenediamine with various carboxylic acids gave benzimidazole derivatives, which were N-alkylated with methyl 4'-(bromomethyl)biphenyl-2-carboxylate to afford the corresponding title com- pounds. Nine novel title compounds were synthesized, and their structures were confirmed by 1H NMR, IR, MS spectra and elemental analyses. And the in vitro preliminary antihypertensive activity was evaluated by the method of aortic ring. Biological screening results demonstrated that some of the compounds displayed potential antihypertensive activity.