Synthesis and aldose reductase inhibitory activity of 7-sulfamoylxanthone-2-carboxylic acids

Abstract
A series of xanthone-2-carboxylic acids substituted in the 7 position with sulfamoyl and other groups was synthesized and assayed in vitro for inhibition of aldose reductase reductase isolated from rabbit lenses. At a concentration of 10-6 M, the N-methyl-N-(2-hydroxyethyl)sulfamoyl derivative produced an 83% inhibition of aldose reductase. The structural requirements for this type of activity are discussed. The compounds were studied for their possible use to prevent cataract formation.