Abstract
Aryl-tetrahydropyridine derivatives were prepared and their PPARalpha/gamma dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARalpha/gamma dual agonist with an EC(50) of 1.73 and 0.64 microM in hPPARalpha and gamma, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Combinatorial Chemistry Techniques
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Diabetes Mellitus, Type 2 / drug therapy
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Disease Models, Animal
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Drug Design
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Mice
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Molecular Structure
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PPAR alpha / agonists*
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PPAR gamma / agonists*
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology*
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Rats
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Rats, Sprague-Dawley
Substances
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PPAR alpha
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PPAR gamma
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Pyridines