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J Med Chem. 2007 Dec 13;50(25):6303-6. Epub 2007 Nov 10.

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.

Author information

1
Merck Research Laboratories, Merck & Co., Inc., Rahway, New Jersey 07065-0900, USA. hong_shen@merck.com

Abstract

Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintaining excellent receptor activity. Compound 2i exhibited good in vivo antilipolytic efficacy while providing a significantly improved therapeutic index over vasodilation (flushing) with respect to niacin in the mouse model.

PMID:
17994679
DOI:
10.1021/jm700942d
[Indexed for MEDLINE]

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