Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Fa-Xiang Ding,Hong C Shen,Larrisa C Wilsie,Mihajlo L Krsmanovic,Andrew K Taggart,Ning Ren,Tian-Quan Cai,Junying Wang,Xinchun Tong,Tom G Holt,Qing Chen,M Gerard Waters,Milton L Hammond,James R Tata,Steven L Colletti

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure–activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles.

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关键词

Agonist,GPR109A,Niacin,Niacin receptor,Cyclohexenamides

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