Abstract
Disalicylic acid derivatives with stilbene and bis-styrylbenzene skeleton were synthesized as PTP1B inhibitors. The most potent in this series exhibited a submicromolar IC(50) value. One of the compounds 7b was tested in an animal model for its efficacy as an anti-diabetic or an anti-obesity agent. In feeding compound 7b to diet-induced obese mice, no significant differences in weight gain and food consumption were observed between the drug-treated and the obese control mice. However, 7b significantly lowered the fasting glucose level and improved the glucose tolerance in the obesity-induced diabetic mice.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Obesity Agents / chemical synthesis
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Anti-Obesity Agents / pharmacology
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Anti-Obesity Agents / therapeutic use*
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Blood Glucose / analysis
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Blood Glucose / metabolism
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Disease Models, Animal
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Fasting
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Glucose Tolerance Test
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Hyperglycemia / drug therapy*
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Mice
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Mice, Inbred C57BL
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Mice, Obese
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Obesity / drug therapy*
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Salicylates / chemical synthesis
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Salicylates / pharmacology
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Salicylates / therapeutic use*
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Stilbenes / chemical synthesis
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Stilbenes / pharmacology
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Stilbenes / therapeutic use*
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Structure-Activity Relationship
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Styrenes / chemical synthesis
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Styrenes / pharmacology
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Styrenes / therapeutic use*
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Weight Gain / drug effects*
Substances
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Anti-Obesity Agents
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Blood Glucose
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Salicylates
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Stilbenes
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Styrenes
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salicylsalicylic acid