Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A

Hong C. Shen,Michael J. Szymonifka,Divya Kharbanda,Qiaolin Deng,Ester Carballo-Jane,Kenneth K. Wu,Tsuei-Ju Wu,Kang Cheng,Ning Ren,Tian-Quan Cai,Andrew K. Taggart,Junying Wang,Xinchun Tong,M. Gerard Waters,Milton L. Hammond,James R. Tata,Steven L. Colletti

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

A urea class of high affinity niacin receptor agonists was discovered. Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q also demonstrated equal affinity to GPR109A as niacin.

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关键词

Niacin,Agonist,Ureas

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