Synthesis and aldose reductase-inhibitory activity of benzo[b]furan derivatives possessing a carboxymethylsulfamoyl group.
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.
Ohishi
Y
Y
Mukai
T
T
Nagahara
M
M
Yajima
M
M
Kajikawa
N
N
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D066298:In Vitro Techniques; D007908:Lens, Crystalline / Q000201:enzymology; D051381:Rats; D013401:Sugar Alcohol Dehydrogenases / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
D001572:Benzofurans; D013449:Sulfonamides; D013401:Sugar Alcohol Dehydrogenases; D000449:Aldehyde Reductase