As a continuation of our efforts directed towards the development of anti-diabetic agents from natural sources, piplartine was isolated from Piper chaba, and was found to inhibit recombinant human ALR2 with an IC(50) of 160 μM. To improve the efficacy, a series of analogues have been synthesized by modification of the styryl/aromatic and heterocyclic ring functionalities of this natural product lead. All the derivatives were tested for their ALR2 inhibitory activity, and results indicated that adducts 3c, 3e and 2j prepared by the Michael addition of piplartine with indole derivatives displayed potent ARI activity, while the other compounds displayed varying degrees of inhibition. The active compounds were also capable of preventing sorbitol accumulation in human red blood cells.

译文

:作为我们致力于从天然来源开发抗糖尿病药的努力的继续,从哌派(Piper chaba)分离了吡哌汀,并发现其抑制重组人ALR2的IC(50)为160μM。为了提高功效,已经通过修饰该天然产物铅的苯乙烯基/芳族和杂环官能团合成了一系列类似物。测试了所有衍生物的ALR2抑制活性,结果表明,通过迈克尔加成的吡哌丁与吲哚衍生物制得的加合物3c,3e和2j表现出有效的ARI活性,而其他化合物则表现出不同程度的抑制作用。活性化合物还能够防止山梨糖醇在人红细胞中积累。

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