Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38

Journal of Medicinal Chemistry

Volumn 58, Issue 17, 2015, Pages 7021-7056

  Becherer, J David ^a   Boros, Eric E ^a   Carpenter, Tiffany Y ^a   Cowan, David J ^a   Deaton, David N ^a   Haffner, Curt D ^a   Jeune, Michael R ^a   Kaldor, Istvan W ^a   Poole, J Chuck ^a   Preugschat, Frank ^a   Rheault, Tara R ^a   Schulte, Christie A ^a   Shearer, Barry G ^a   Shearer, Todd W ^a   Shewchuk, Lisa M ^a   Smalley, Terrence L ^a   Stewart, Eugene L ^a   Stuart, J Darren ^a   Ulrich, John C ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL 4 ((3 METHYLBENZYL)AMINO)QUINOLINE 8 CARBOXAMIDE; 2 METHYL 4 ((4 METHYLBENZYL)AMINO)QUINOLINE 8 CARBOXAMIDE; 2 METHYL 4 (2 METHYLBENZYLAMINO)QUINOLINE 8 CARBONITRILE; 2 METHYL 4 (2 METHYLBENZYLAMINO)QUINOLINE 8 CARBOXAMIDE; 2 METHYL 4 [[(2,3,6 TRICHLOROPHENYL)METHYL]AMINO] 8 QUINOLINECARBOXAMIDE; 4 ((2 FLUORO 6 (TRIFLUOROMETHYL)BENZYL)AMINO) 2 METHYLQUINOLINE 8 CARBOXAMIDE; 4 ((2 METHOXYBENZYL)AMINO) 2 METHYLQUINOLINE 8 CARBOXAMIDE; 4 ((3 METHOXYBENZYL)AMINO) 2 METHYLQUINOLINE 8 CARBOXAMIDE; 4 (4 CHLOROBENZYLAMINO) 2 METHYLQUINOLINE 8 CARBONITRILE; 4 (BENZYLAMINO) 2 METHYLQUINOLINE 8 CARBONITRILE; 4 (BENZYLAMINO) 2 METHYLQUINOLINE 8 CARBOXAMIDE; 4 AMINO 2 METHYL 8 QUINOLINECARBOXAMIDE; 4 AMINOQUINOLINE DERIVATIVE; 4 HYDROXY 2 METHYLQUINOLINE 8 CARBONITRILE; 4 [[(2,3 DICHLOROPHENYL)METHYL]AMINO] 2 METHYL 8 QUINOLINECARBOXAMIDE; 4 [[(3 CHLOROPHENYL)METHYL]AMINO] 2 METHYL 8 QUINOLINECARBOXAMIDE; 4[[(2,6 DIMETHYLPHENYL)METHYL]AMINO] 2 METHYL 8 QUINOLINECARBOXAMIDE; 8 BROMO 2 METHYL N (3 METHYLBENZYL)QUINOLIN 4 AMINE; 8 BROMO 2 METHYL N (4 METHYLBENZYL)QUINOLIN 4 AMINE; 8 BROMO N (2 METHOXYBENZYL) 2 METHYLQUINOLIN 4 AMINE; 8 BROMO N (3 METHOXYBENZYL) 2 METHYLQUINOLIN 4 AMINE; 8 BROMO N (4 METHOXYBENZYL) 2 METHYLQUINOLIN 4 AMINE; 8 BROMO N [(2,6 DIMETHYLPHENYL)METHYL] 2 METHYL 4 QUINOLINAMINE; 8 BROMO N [(3 CHLOROPHENYL)METHYL] 2 METHYL 4 QUINOLINAMINE; 8 CYANO 2 METHYLQUINOLIN 4 YL TRIFLUOROMETHANESULFONATE; AMIDE; CD38 ANTIGEN; ENZYME INHIBITOR; N BENZYL 8 BROMO 2 METHYLQUINOLIN 4 AMINE; NICOTINAMIDE ADENINE DINUCLEOTIDE; UNCLASSIFIED DRUG; 2-METHYL-4-(((2,3,6-TRICHLOROPHENYL)METHYL)AMINO)-8-QUINOLINECARBOXAMIDE; 4-((2-FLUORO-6-(TRIFLUOROMETHYL)BENZYL)AMINO)-2-METHYLQUINOLINE-8-CARBOXAMIDE; AMINOQUINOLINE DERIVATIVE; ARTIFICIAL MEMBRANE; QUINOLINE DERIVATIVE;

ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; C57BL 6 MOUSE; CONTROLLED STUDY; DIET INDUCED OBESITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; IN VIVO STUDY; MOUSE; NONHUMAN; PHARMACOKINETIC PARAMETERS; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; ARTIFICIAL MEMBRANE; BIOAVAILABILITY; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; HUMAN; HYDROLYSIS; LIVER; METABOLISM; OBESITY; PERMEABILITY; PROTEIN CONFORMATION; SKELETAL MUSCLE; STEREOISOMERISM; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

AMIDES; AMINOQUINOLINES; ANIMALS; ANTIGENS, CD38; BIOLOGICAL AVAILABILITY; CRYSTALLOGRAPHY, X-RAY; HUMANS; HYDROLYSIS; LIVER; MEMBRANES, ARTIFICIAL; MICE, INBRED C57BL; MODELS, MOLECULAR; MUSCLE, SKELETAL; NAD; OBESITY; PERMEABILITY; PROTEIN CONFORMATION; QUINOLINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84941595521     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00992     Document Type: Article

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