Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675)

Journal of Medicinal Chemistry

Volumn 53, Issue 9, 2010, Pages 3618-3625

  Haynes, Nancy Ellen ^a   Corbett, Wendy L ^a   Bizzarro, Fred T ^a   Guertin, Kevin R ^a   Hilliard, Darryl W ^a   Holland, George W ^a   Kester, Robert F ^a   Mahaney, Paige E ^a   Qi, Lida ^a   Spence, Cheryl L ^a   Tengi, John ^a   Dvorozniak, Mark T ^a   Railkar, Aruna ^a   Matschinsky, Franz M ^b   Grippo, Joseph F ^a   Grimsby, Joseph ^a   Sarabu, Ramakanth ^a  

^a HOFFMANN LA ROCHE INC   (United States)

^b UNIVERSITY OF PENNSYLVANIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 CYCLOPENTYL 2 ( 4 METHANESULFONYLPHENYL) N THIAZOL 2 YL PROPIONAMIDE; ENZYME ACTIVATOR; GLUCOKINASE ACTIVATOR; PROPIONAMIDE DERIVATIVE; RO 0274375; RO 0281675; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ALLOSTERISM; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SCREENING; DRUG TARGETING; HUMAN; HUMAN EXPERIMENT; HYPOGLYCEMIA; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MOLECULE; MOUSE; NONHUMAN; NORMAL HUMAN; PHARMACOLOGICAL PARAMETERS; RAT; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

ANIMALS; BLOOD GLUCOSE; CELL LINE; CYTOTOXINS; DIABETES MELLITUS, TYPE 2; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; GLUCOKINASE; HUMANS; HYPOGLYCEMIC AGENTS; INSULIN; MALE; MICE; PHARMACOKINETICS; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; THIAZOLES;

EID: 77952064740     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100039a     Document Type: Article

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