Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A
作者: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
DOI:10.1016/j.bmcl.2007.10.055
日期:2007.12
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 demonstrated equal affinity to GPR109A as niacin. (c) 2007 Elsevier Ltd. All rights reserved.