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Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. Epub 2007 Oct 18.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA. hong_shen@merck.com

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.

PMID:
18029181
DOI:
10.1016/j.bmcl.2007.10.055
[Indexed for MEDLINE]

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