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

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• 作者：Hee Oon Han ; Seung Hae Kim ; Kyoung-Hee Kim ; Gwong-Cheung Hur ; Hyeon Joo Yim ; Hee-Kyung Chung ; Sung Ho Woo ; Ki Dong Koo ; Chang-Seok Lee ; Jong Sung Koh ; et al.
• 关键词：PPAR ; Dual agonist ; Oxime ; Propanoic acid
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 February 2007
• 卷：17
• 期：4
• 页码：937-941
• 文件大小：223 K

摘要

Oxime ethers of α-acyl-β-phenylpropanoic acids were prepared to apply as PPARα and γ dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC₅₀ of 19 and 13 nM in PPARα and γ, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.