A series of 17 compounds were synthesized based on the premise that the minimal pharmacophore for aldose reductase inhibition requires the presence of both an aryl group and polar group connected by a linking structure. Three groups of compounds were synthesized, the first possessing an aniline-4-(2'-6'-methylbenzothiazole) or 2-aminobenzothiazole group as the aryl group, the second possessing a 2-naphthyl
基于以下前提合成了一系列17种化合物,前提是抑制醛糖还原酶的最小药效团需要同时存在通过连接结构连接的芳基和极性基团。合成了三组化合物,第一组具有
苯胺-4-(2'-6'-甲基
苯并噻唑)或
2-氨基苯并噻唑基作为芳基,第二组具有2-
萘基作为芳基,第三组具有任一4-(
2-苯基噻唑)或2-(5-2'-
硝基苯基
呋喃)作为芳基。在所有这三个基团中,
羧酸盐或其甲酯通过各种长度的亚甲基碳和酰胺或肉桂酰胺基与芳基连接。当羧基通过长度为五个原子的连接结构与芳基分开时,观察到最佳活性。