Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus

Journal of Medicinal Chemistry

Volumn 55, Issue 3, 2012, Pages 1318-1333

  Pfefferkorn, Jeffrey A ^a   Guzman Perez, Angel ^a   Litchfield, John ^a   Aiello, Robert ^a   Treadway, Judith L ^a   Pettersen, John ^a   Minich, Martha L ^a   Filipski, Kevin J ^a   Jones, Christopher S ^a   Tu, Meihua ^a   Aspnes, Gary ^a   Risley, Hud ^a   Bian, Jianwei ^a   Stevens, Benjamin D ^a   Bourassa, Patricia ^a   D'Aquila, Theresa ^a   Baker, Levenia ^a   Barucci, Nicole ^a   Robertson, Alan S ^a   Bourbonais, Francis ^a   Derksen, David R ^a   MacDougall, Margit ^a   Cabrera, Over ^a   Chen, Jing ^a   Lapworth, Amanda Lee ^a   Landro, James A ^a   Zavadoski, William J ^a   Atkinson, Karen ^a   Haddish Berhane, Nahor ^a   Tan, Beijing ^a   Yao, Lili ^a   Kosa, Rachel E ^a   Varma, Manthena V ^a   Feng, Bo ^a   Duignan, David B ^a   El Kattan, Ayman ^a   Murdande, Sharad ^a   Liu, Shenping ^a   Ammirati, Mark ^a   Knafels, John ^a   Dasilva Jardine, Paul ^a   Sweet, Laurel ^a   Liras, Spiros ^a   Rolph, Timothy P ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 [3 CYCLOPENTYL 2 [4 (TRIFLUOROMETHYL) 1H IMIDAZOL 1 YL]PROPANAMIDO]NICOTINIC ACID; ANTIDIABETIC AGENT; CARBOXYLIC ACID; GLUCOKINASE; ORGANIC ANION TRANSPORTER; UNCLASSIFIED DRUG;

ANTIDIABETIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG SYNTHESIS; LIVER CELL; NON INSULIN DEPENDENT DIABETES MELLITUS; PANCREAS ISLET BETA CELL; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC SITE; ANIMALS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DOGS; ENZYME ACTIVATORS; GLUCOKINASE; HAPLORHINI; HEPATOCYTES; HUMANS; HYPOGLYCEMIC AGENTS; IMIDAZOLES; INSULIN-SECRETING CELLS; MALE; MODELS, MOLECULAR; NICOTINIC ACIDS; ORGANIC ANION TRANSPORTERS; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RATS, WISTAR; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION;

EID: 84863115976     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2014887     Document Type: Article

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