Abstract
Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to apply as PPARalpha and gamma dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in PPARalpha and gamma, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.
MeSH terms
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Animals
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Area Under Curve
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Biological Availability
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Blood Glucose / metabolism
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Cell Line, Tumor
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Drug Design
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Humans
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacokinetics
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Hypoglycemic Agents / pharmacology*
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Indicators and Reagents
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Lipids / blood
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Models, Molecular
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PPAR alpha / agonists*
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PPAR gamma / agonists*
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Phenylpropionates / chemical synthesis*
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Phenylpropionates / pharmacology*
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Rosiglitazone
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Structure-Activity Relationship
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Thiazolidinediones / pharmacology
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Triglycerides / blood
Substances
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Blood Glucose
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Hypoglycemic Agents
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Indicators and Reagents
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Lipids
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PPAR alpha
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PPAR gamma
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Phenylpropionates
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Thiazolidinediones
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Triglycerides
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Rosiglitazone