4.5 Article

Design and synthesis of oxime ethers of α-acyl-β-phenylpropanoic acids as PPAR dual agonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 4, Pages 937-941

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.11.050

Keywords

PPAR; dual agonist; oxime; propanoic acid

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Oxime ethers of alpha-acyl-(3-phenylpropanoic acids were prepared to apply as PPAR alpha and gamma dual agonists. Among them, compound 111 proved to exhibit potent in vitro activities with EC50 of 19 and 13 nM in PPAR alpha and gamma, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in dbldb mice model. (c) 2006 Elsevier Ltd. All rights reserved.

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