Abstract
Several methyl benzothiazolyloxybenzoates, S-isosters, and the corresponding benzoic acids were synthesized and tested as aldose reductase inhibitors (ARIs). Out of this series, the ester derivative 2a-7 was found to exhibit the highest enzyme-inhibitoric activity. In order to investigate this unexpected result, further modifications were carried out which allowed us to explain this finding and to open a path to a novel class of ARIs.
MeSH terms
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Aldehyde Reductase / antagonists & inhibitors*
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Animals
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Benzoic Acid / chemical synthesis*
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Benzoic Acid / chemistry
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Benzoic Acid / pharmacology
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Benzothiazoles
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Cattle
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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In Vitro Techniques
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Lens, Crystalline / enzymology
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Molecular Structure
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Structure-Activity Relationship
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Thiazoles / chemistry*
Substances
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Benzothiazoles
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Enzyme Inhibitors
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Thiazoles
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Benzoic Acid
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Aldehyde Reductase
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benzothiazole