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Peer-reviewed veterinary case report

Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2008
Authors:
Kim, Eunkyung et al.
Affiliation:
Yuhan Research Institute · South Korea
Species:
rodent

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.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/18771917/