Abstract
Propionic acid derivative 8, which was designed and synthesized based on putative pharmacophores of known PPARgamma- and PPARalpha-selective compounds, exhibits potent dual PPARalpha/gamma agonist activity as demonstrated by in vitro binding and dose overlap in the newly introduced EOB mouse model for glucose lowering and lipid/cholesterol homeostasis.
MeSH terms
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Animals
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Blood Glucose / metabolism
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Cholesterol, HDL / blood
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Diabetes Mellitus / blood
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Diabetes Mellitus / drug therapy
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Diabetes Mellitus / genetics
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Diabetes Mellitus, Type 2 / drug therapy
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Drug Design
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacology*
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Mice
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Mice, Inbred Strains
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Propionates / chemical synthesis*
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Propionates / pharmacology*
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Receptors, Cytoplasmic and Nuclear / agonists*
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Receptors, Cytoplasmic and Nuclear / genetics
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Transcription Factors / agonists*
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Transcription Factors / genetics
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Triglycerides / blood
Substances
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Blood Glucose
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Cholesterol, HDL
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Hypoglycemic Agents
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Propionates
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Receptors, Cytoplasmic and Nuclear
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Transcription Factors
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Triglycerides