Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor

Journal of Medicinal Chemistry

Volumn 50, Issue 25, 2007, Pages 6356-6366

  Tran, Joe A ^a   Jiang, Wanlong ^a   Tucci, Fabio C ^a,b   Fleck, Beth A ^a   Wen, Jenny ^a   Sai, Yang ^a   Madan, Ajay ^a   Ta, Kung Chen ^a   Markison, Stacy ^a   Foster, Alan C ^a   Hoare, Sam R ^a   Marks, Daniel ^a,c   Harman, John ^a   Chen, Caroline W ^a   Arellano, Melissa ^a   Marinkovic, Dragan ^a   Bozigian, Haig ^a   Saunders, John ^a,d   Chen, Chen ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

^b Tanabe Research Laboratories   (United States)

^c OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

^d VERTEX PHARMACEUTICALS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 [3 [1 AMINO 3 METHYLBUTYL] 2 PYRIDINYL] 4 [2 METHYL 3 (2,4 DICHLOROPHENYL)PROPIONYL]PIPERAZINE TRIFLUOROACETATE; 1 [3 [1 AMINO 3 METHYLBUTYL] 6 METHYL 2 PYRIDINYL] 4 [METHYL 3 (2,4 DICHLOROPHENYL)PROPIONYL]PIPERAZINE TRIFLUOROACETATE; 1 [3 [AMINO 3 METHYLBUTYL] 2 PYRIDINYL] 4 [3 (2,4 DICHLOROPHENYL)PROPIONYL]PIPERAZINE TRIFLUOROACETATE; 2 [4 [3 (2,4 DICHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL 5 TRIFLUOROMETHYL)PHENYL] 3 METHYLBUTYLAMINE TRIFLUOROACETATE; [2 [4 [(2 OXO 1 PYRROLIDINYL) 3 (2,4 DICHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 3 FLUOROPHENYL] 3 METHYLBUTYLAMINE; [2 [4 [2 METHYL 3 (2 METHOXY 4 CHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 5 (TRIFLUOROMETHYL)PHENYL] 3 METHYLBUTYLAMINE MESYLATE; [2 [4 [METHYL 3 (4 CHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 5 METHYLPHENYL] 3 METHYLBUTYLAMINE MESYLATE; BENZYLAMINE DERIVATIVE; MELANOCORTIN 4 RECEPTOR; N (1 AMINOETHYL) N [[2 [4 [(2 OXO 1 PYRROLIDINYL) 3 (2,4 DICHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 3 FLUOROPHENYL] 3 METHYLBUTYL]AMINE MESYLATE; N [1 [2 [4 [3 (2,4 DICHLOROPHENYL) 2 (2 OXO 1 PYRROLIDINYL)PROPIONYL] 1 PIPERAZINYL] 5 METHYLPHENYL] 3 METHYLBUTYL] 3 (DIMETHYLAMINO)PROPANAMIDE MESYLATE; N [[2 [4 [3 (4 CHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 5 (TRIFLUOROMETHYL)PHENYL] 3 METHYLBUTYL] 2 AMINOACETAMIDE; N [[2 [4 [METHYL 3 (2,4 DICHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 3 PYRIDINYL] 3 METHYLBUTYL] 2 AMINOACETAMIDE MESYLATE TRIFLUOROACETATE; N [[2 [4 [METHYL 3 (2,4 DICHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 6 METHYL 3 PYRIDINYL] 3 METHYLBUTYL] 3 (DIMETHYLAMINO)PROPIONAMIDE; N [[2 [4 [METHYL 3 (4 CHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 5 CHLOROPHENYL] 3 METHYLBUTYL] 3 (DIMETHYLAMINO)PROPIONAMIDE; N [[2 [4 [METHYL 3 (4 CHLOROPHENYL)PROPIONYL] 1 PIPERAZINYL] 5 METHYLPHENYL] 3 METHYLBUTYL] 3 (DIMETHYLAMINO)PROPIONAMIDE MESYLATE; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CACHEXIA; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG EFFICACY; DRUG MEGADOSE; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FOOD INTAKE; HUMAN; HUMAN CELL; LEAN BODY WEIGHT; MALE; MOUSE; NONHUMAN; RAT; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; BENZYLAMINES; CACHEXIA; CARCINOMA, LEWIS LUNG; CELL LINE; CRYSTALLOGRAPHY, X-RAY; CYCLIC AMP; DRUG DESIGN; EATING; HUMANS; MALE; MICE; MICE, INBRED C57BL; MODELS, MOLECULAR; NEOPLASM TRANSPLANTATION; PIPERAZINES; PYRIDINES; RECEPTOR, MELANOCORTIN, TYPE 4; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 37049016920     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm701137s     Document Type: Article

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