2－烷基－3－取代－3H－咪唑并［4，5－b］吡啶类衍生物的合成及生物活性

Synthesis and Bio-activity of 2-Alkyl-3-Substituted-3H-Imidazo[4,5-b]pyridines

为寻找新的非肽类血管紧张素Ⅱ受体拮抗剂，以Ｌ－１５８，８０９为先导，结合生物电子等排原理，利用计算机辅助分子结构模拟研究结果，设计并合成了８个２－烷基－３－取代－３Ｈ－咪唑并吡啶类衍生物。所有目的化合物均未见文献报道，其结构经红外光谱、核磁共振氢谱和质谱确证。初步药理实验表明，化合物２ｌｃ具有一定的抗高血压活性。

Nonpeptide Ang Ⅱ receptor antagonists are orally bio-available and possess good antihypertensive activity with a long duration of action.In order to search for the new drug with high potency, derived from the lead compound L-158, 809, and based on the principle of bioisoterism and the result of computer-assisted molecular medeling study, a series of 2-alkyl-3-substituted-3H-imidazo[4,5-b]pyridines are designed and synthesized.All the eight target compounds are thus far unreported and now identified by 1R,￣1HNMR and MS spectrum.Of all the compounds tested,compound 21c is shown to have an antihypertensive activity.