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 isolated from rabbit lenses. At a concentration of 10(-6) M, the N-methyl-N-(2-hydroxyethyl)sulfamoyl derivative 14 produced an 83% inhibition of aldose reductase. The structural requirements for this type of activity are discussed.
MeSH terms
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Aldehyde Reductase / antagonists & inhibitors*
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Animals
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Chemical Phenomena
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Chemistry
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Kinetics
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Lens, Crystalline / enzymology
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Male
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Rabbits
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Structure-Activity Relationship
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Sugar Alcohol Dehydrogenases / antagonists & inhibitors*
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Sulfones / chemical synthesis*
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Sulfones / pharmacology
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Xanthenes / chemical synthesis*
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Xanthenes / pharmacology
Substances
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Sulfones
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Xanthenes
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Sugar Alcohol Dehydrogenases
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Aldehyde Reductase