Abstract
A series of 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles has been synthesized and tested for PPARgamma agonist activity. SAR were developed and revealed that 6-acyl-2(3H)-benzothiazolone derivatives with 1,3-dicarbonyl group were the most potent. IP administration of compound 22 exhibited comparable levels of glucose and triglyceride correction to PO administration of rosiglitazone in the ob/ob mouse studies.
MeSH terms
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Animals
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Azo Compounds / chemical synthesis*
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Azo Compounds / chemistry
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Azo Compounds / pharmacology*
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Binding Sites
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Cell Line
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Drug Design
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Female
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology*
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Humans
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Male
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Mice
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Mice, Inbred C57BL
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Models, Molecular
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Molecular Structure
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PPAR gamma / agonists*
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PPAR gamma / chemistry
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PPAR gamma / metabolism
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Structure-Activity Relationship
Substances
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Azo Compounds
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Heterocyclic Compounds
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PPAR gamma