The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 9, 2011, Pages 2721-2724

  Imbriglio, Jason E ^a   Dirocco, Daniel ^a   Bodner, Rena ^a   Raghavan, Subharekha ^a   Chen, Weichun ^a   Marley, Daria ^a   Esser, Craig ^a   Holt, Tom G ^a   Wolff, Michael S ^a   Taggart, Andrew K P ^a   Waters, M Gerard ^a   Tata, James R ^a   Colletti, Steven L ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Anthranilic acid; Atherosclerosis; Niacin

Indexed keywords

AMINOANTHRANILIC ACID DERIVATIVE; ANTHRANILIC ACID DERIVATIVE; G PROTEIN COUPLED RECEPTOR; GPR 109A PROTEIN; NICOTINIC ACID; UNCLASSIFIED DRUG;

CONFERENCE PAPER; DOWN REGULATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG MECHANISM; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; FLUSHING; NONHUMAN; RECEPTOR AFFINITY; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

ANIMALS; DRUG DISCOVERY; FLUORINE; HUMANS; INHIBITORY CONCENTRATION 50; MICE; MOLECULAR STRUCTURE; NIACIN; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, NICOTINIC;

EID: 79955466022     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.116     Document Type: Conference Paper

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12. For details on the synthesis of the disclosed agonists refer to WO2007075749A2.