- Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Bioorganic & medicinal chemistry letters (2007-11-22)
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
PMID18029181
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 demonstrated equal affinity to GPR109A as niacin.