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首页> 外文期刊>Bulletin of the Korean Chemical Society >Design and Synthesis of Oxime Ethers of β-Oxo-γ-phenylbutanoic Acids as PPAR α and -γ Dual Agonists
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Design and Synthesis of Oxime Ethers of β-Oxo-γ-phenylbutanoic Acids as PPAR α and -γ Dual Agonists

机译:β-氧代-γ-苯基丁酸作为PPARα和-γ双激动剂的肟醚的设计与合成

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摘要

Oxime ethers of β-oxo-γ-phenylbutanoic acids were prepared to develop more effective PPAR α and γ dual agonists. Among them, compound 11k exhibited potent in vitro activities with EC50 of 2.5 nM and 3.3 nM in PPAR α and γ, respectively. It showed better glucose lowering effects than rosiglitazone 1 and improved the lipid profile like plasma triglyceride in db/db mice model.
机译:制备了β-氧代-γ-苯基丁酸的肟醚,以开发更有效的PPARα和γ双激动剂。其中,化合物11k在PPARα和γ中表现出有效的体外活性,EC50分别为2.5 nM和3.3 nM。它显示出比罗格列酮1更好的降糖效果,并改善了db / db小鼠模型中的脂质分布,如血浆甘油三酸酯。

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