具有羧甲基氨磺酰基的苯并[b]呋喃衍生物的合成及其醛糖还原酶抑制活性

Synthesis and aldose reductase-inhibitory activity of benzo[b]furan derivatives possessing a carboxymethylsulfamoyl group.

作者信息

Ohishi Y, Mukai T, Nagahara M, Yajima M, Kajikawa N

出版信息

Chem Pharm Bull (Tokyo). 1989 Sep;37(9):2398-405. doi: 10.1248/cpb.37.2398.

DOI:10.1248/cpb.37.2398

Abstract

Various benzo[b]furan derivatives with a carboxymethylsulfamoyl group were prepared and evaluated for aldose reductase-inhibitory potency. Most of the compounds displayed significant inhibitory activities (IC50, 10(-8)-10(-7) M). Among the test compounds, the compounds having a carboxymethylsulfamoyl group at the 3- or 4-position exhibited the greatest inhibitory potency. Structure-activity trends of the tested compounds are discussed.

摘要

制备了各种带有羧甲基氨磺酰基的苯并[b]呋喃衍生物，并对其醛糖还原酶抑制活性进行了评估。大多数化合物表现出显著的抑制活性（IC50，10^(-8)-10^(-7) M）。在测试化合物中，在3-或4-位带有羧甲基氨磺酰基的化合物表现出最大的抑制活性。讨论了测试化合物的构效关系趋势。