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Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A |
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| Authors: | Shen Hong C Szymonifka Michael J Kharbanda Divya Deng Qiaolin Carballo-Jane Ester Wu Kenneth K Wu Tsuei-Ju Cheng Kang Ren Ning Cai Tian-Quan Taggart Andrew K Wang Junying Tong Xinchun Waters M Gerard Hammond Milton L Tata James R Colletti Steven L |
| Affiliation: | aDepartment of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA bDepartment of Pharmacology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA cDepartment of Cardiovascular Diseases, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA dDepartment of Drug metabolism, Merck Research Laboratories, P.O. Box 2000, Rahway, NJ 07065-0900, USA |
| Abstract: | 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. |
| Keywords: | Niacin Agonist Ureas |
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