Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 15, 2007, Pages 5166-5176

  Tran, Joe A ^a   Tucci, Fabio C ^a   Jiang, Wanlong ^a   Marinkovic, Dragan ^a   Chen, Caroline W ^a   Arellano, Melissa ^a   Markison, Stacy ^a   Fleck, Beth A ^a   Wen, Jenny ^a   White, Nicole S ^a   Pontillo, Joseph ^a   Saunders, John ^a   Marks, Daniel ^b   Hoare, Sam R ^a   Madan, Ajay ^a   Foster, Alan C ^a   Chen, Chen ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

^b OREGON HEALTH AND SCIENCE UNIVERSITY   (United States)

Author keywords

Animal model; Antagonist; Cachexia; Melanocortin 4 receptor; Pharmacokinetics; Pyrrolidinone; Synthesis

Indexed keywords

1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 FLUOROPHENYL]PIPERAZIN 1 YL] 1 (2,4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL]PIPERAZIN 1 YL] 1 (2,4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE MESYLATE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL]PIPERAZIN 1 YL] 1 (2,4-DICHLOROBENZYL) 2 OXOETHYL]PIPERAZIN 2 ONE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL]PIPERAZIN 1 YL] 1 (4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE MESYLATE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL]PIPERAZIN 1 YL] 1 (4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE TRIFLUOROACETATE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL) 6 FLUOROPHENYL]PIPERAZIN 1 YL] 1 (2,4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL)PHENYL]PIPERAZIN 1 YL] 1 (2,4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE; 1 [2 [4 [2 (1 AMINO 3 METHYLBUTYL)PHENYL]PIPERAZIN 1 YL] 1 (4 DICHLOROBENZYL) 2 OXOETHYL]PYRROLIDIN 2 ONE MESYLATE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 FLUOROPHENYL] 4 [ACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL] 4 [(PIPERIDIN 4 YLCARBOXAMIDO) 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE TRIFLUOROACETATE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL] 4 [ACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL] 4 [AMINO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 4 TRIFLUOROMETHYLPHENYL] 4 [AMINOACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 6 FLUOROPHENYL) 4 [AMINOACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE TRIFLUOROACETATE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 6 FLUOROPHENYL] 4 [ACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE TRIFLUOROACETATE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 6 TRIFLUOROMETHYLPHENYL] 4 [ACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (1 AMINO 3 METHYLBUTYL) 6 TRIFLUOROMETHYLPHENYL] 4 [AMINOACETAMIDO 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE TRIFLUOROACETATE; 1 [4 [2 (AMINO 3 METHYLBUTYL) 4 FLUOROPHENYL] 4 [(3 AMINOPROPIONYLAMIDO) 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (AMINO 3 METHYLBUTYL) 6 FLUOROPHENYL] 4 [(3 AMINOPROPIONYLAMIDO) 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE; 1 [4 [2 (AMINO 3 METHYLBUTYL) 6 TRIFLUOROMETHYLPHENYL] 4 [(3 AMINOPROPIONYLAMIDO) 3 (2,4 DICHLOROPHENYL)PROPIONYL]]PIPERAZINE TRIFLUOROACETATE; MELANOCORTIN 4 RECEPTOR; PHENYLALANINE DERIVATIVE; PYRROLIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CACHEXIA; CONTROLLED STUDY; DISEASE MODEL; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; IN VIVO STUDY; MALE; MOUSE; NONHUMAN;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BODY COMPOSITION; BODY WEIGHT; CACHEXIA; DISEASE MODELS, ANIMAL; HUMANS; MALE; MICE; MICE, INBRED C57BL; MOLECULAR STRUCTURE; PYRROLIDINONES; RECEPTOR, MELANOCORTIN, TYPE 4; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA; MURINAE;

EID: 34249939200     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2007.05.026     Document Type: Article

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