Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 9, 2009, Pages 2400-2403

  Humphries, Paul S ^a   Benbow, John W ^a   Bonin, Paul D ^a   Boyer, David ^a   Doran, Shawn D ^a   Frisbie, Richard K ^a   Piotrowski, David W ^a   Balan, Gayatri ^a   Bechle, Bruce M ^a   Conn, Edward L ^a   Dirico, Kenneth J ^a   Oliver, Robert M ^a   Soeller, Walter C ^a   Southers, James A ^a   Yang, Xiaojing ^a  

^a PFIZER INC   (United States)

Author keywords

Diabetes; GPR40; Ligand efficiency; Tetrahydroisoquinolinones

Indexed keywords

G PROTEIN COUPLED RECEPTOR; TETRAHYDROISOQUINOLINE DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; DRUG ACTIVITY; DRUG CLEARANCE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; IN VITRO STUDY; IN VIVO STUDY; LIVER BLOOD FLOW; MALE; MICROSOME MEMBRANE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; CHEMISTRY, PHARMACEUTICAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMANS; INHIBITORY CONCENTRATION 50; LIGANDS; METABOLIC CLEARANCE RATE; MODELS, CHEMICAL; RATS; RECEPTORS, G-PROTEIN-COUPLED; STRUCTURE-ACTIVITY RELATIONSHIP; TETRAHYDROISOQUINOLINES;

RATTUS;

EID: 64249111493     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.082     Document Type: Article

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