Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 4, 2013, Pages 979-992

  Taygerly, Joshua P ^a   McGee, Lawrence R ^a   Rubenstein, Steven M ^a   Houze, Jonathan B ^a   Cushing, Timothy D ^a   Li, Yang ^a   Motani, Alykhan ^a   Chen, Jin Long ^a   Frankmoelle, Walter ^a   Ye, Guosen ^a   Learned, Marc R ^a   Jaen, Juan ^a   Miao, Shichang ^a   Timmermans, Pieter B ^a   Thoolen, Martin ^a   Kearney, Patrick ^a   Flygare, John ^a   Beckmann, Holger ^a   Weiszmann, Jennifer ^a   Lindstrom, Michelle ^a   Walker, Nigel ^a   Liu, Jinsong ^a   Biermann, Donna ^a   Wang, Zhulun ^a   Hagiwara, Atsushi ^b   Iida, Tetsuya ^b   Aramaki, Hisateru ^b   Kitao, Yuki ^b   Shinkai, Hisashi ^b   Furukawa, Noboru ^b   Nishiu, Jun ^b   Nakamura, Motonao ^b   more..

^a AMGEN INC   (United States)

^b Japan Tobacco 2 1 ^*  (Japan)

Author keywords

INT131; PPAR ; Selective PPAR modulator; SPPAR Ms; Type 2 diabetes

Indexed keywords

2 (5 CHLOROPYRIDIN 3 YLOXY) 5 (2,4 DICHLORO 5 METHYLPHENYLSULFONAMIDO) N ETHYLBENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) 5 (2,4 DICHLOROPHENYLSULFONAMIDO) N ETHYLBENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) 5 (3,4 DICHLOROPHENYLSULFONAMIDO) N ETHYLBENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYL 5 (4 IODOPHENYLSULFONAMIDO)BENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYL 5 (4 METHOXYPHENYLSULFONAMIDO)BENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYL 5 (4 NITROPHENYLSULFONAMIDO)BENZAMIDE; 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYL 5 [4 (METHYLSULFONYL)PHENYLSULFONAMIDO]BENZAMIDE; 2 CHLORO N [3,5 DICHLORO 4 (QUINOLIN 3 YLOXY)PHENYL] 4 (TRIFLUOROMETHYL)BENZENESULFONAMIDE; 2,4 DICHLORO N [3 CHLORO 4 (5 CHLOROPYRIDIN 3 YLOXY)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [3 CHLORO 4 (QUINOLIN 3 YLOXY)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [3 FLUORO 4 (QUINOLIN 3 YLOXY)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [3,5 DICHLORO 4 (QUINOLIN 3 YLOXY)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 (METHYLSULFONYL)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 (TRIFLUOROMETHYL)PHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 CYANOPHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 FLUOROPHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 METHOXYPHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY) 3 METHYLPHENYL]BENZENESULFONAMIDE; 2,4 DICHLORO N [4 (5 CHLOROPYRIDIN 3 YLOXY)PHENYL]BENZENESULFONAMIDE; 5 (4 TERT BUTYLPHENYLSULFONAMIDO) 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYLBENZAMIDE; 5 [2 CHLORO 4 (TRIFLUOROMETHYL)PHENYLSULFONAMIDO] 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYLBENZAMIDE; 5 [4 BROMO 2 (TRIFLUOROMETHYL)PHENYLSULFONAMIDO] 2 (5 CHLOROPYRIDIN 3 YLOXY) N ETHYLBENZAMIDE; ANTIDIABETIC AGENT; INT 131; N [3 ACETYL 4 (5 CHLOROPYRIDIN 3 YLOXY)PHENYL] 2,4 DICHLOROBENZENESULFONAMIDE; N [3 ACETYL 4 (QUINOLIN 3 YLOXY)PHENYL] 2,4 DICHLOROBENZENESULFONAMIDE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PIOGLITAZONE; ROSIGLITAZONE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIDIARRHEAL ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; INSULIN SENSITIVITY; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; STRUCTURE ACTIVITY RELATION; TREATMENT RESPONSE;

ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 ENZYME SYSTEM; DIABETES MELLITUS, EXPERIMENTAL; HALF-LIFE; INSULIN RESISTANCE; MALE; MICE; PPAR GAMMA; PROTEIN STRUCTURE, TERTIARY; QUINOLINES; RATS; RATS, SPRAGUE-DAWLEY; RATS, ZUCKER; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

RODENTIA;

EID: 84873285630     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.11.058     Document Type: Article

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