Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 11, 2010, Pages 3372-3375

  Ding, Fa Xiang ^a   Shen, Hong C ^a   Wilsie, Larrisa C ^a   Krsmanovic, Mihajlo L ^a   Taggart, Andrew K ^a   Ren, Ning ^a   Cai, Tian Quan ^a   Wang, Junying ^a   Tong, Xinchun ^a   Holt, Tom G ^a   Chen, Qing ^a   Gerard Waters, M ^a   Hammond, Milton L ^a   Tata, James R ^a   Colletti, Steven L ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Agonist; Cyclohexenamides; GPR109A; Niacin; Niacin receptor

Indexed keywords

CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; NICOTINIC ACID; NICOTINIC ACID DERIVATIVE; PYRAZOLYL PROPIONYL CYCLOHEXENAMIDE DERIVATIVE; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; MAXIMUM PLASMA CONCENTRATION; RECEPTOR AFFINITY; SERUM; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; CYCLOHEXENES; MICE; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77953289793     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.013     Document Type: Article

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