Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 1, 2008, Pages 129-136

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

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

Agonist; Animal model; Antagonist; Melanocortin 4 receptor; Obesity; Potency; Pyrrolidine; Stereochemistry

Indexed keywords

4 PHENYLPYRROLIDINE 3 CARBOXAMIDE ERIVATIVE; FENFLURAMINE; MELANOCORTIN 4 RECEPTOR; MELANOCORTIN 4 RECEPTOR AGONIST; MELANOCORTIN 4 RECEPTOR ANTAGONIST; PYRROLIDINE DERIVATIVE; TETRAHYDROPYRAN DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; CELL STRAIN CACO 2; CELL STRAIN HEK293; CONTROLLED STUDY; DIASTEREOISOMER; DISEASE MODEL; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IC 50; MALE; NONHUMAN; OBESITY; RAT; RECEPTOR AFFINITY; STRUCTURE ANALYSIS; TRANS ISOMER;

AMIDES; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; EATING; HUMANS; KINETICS; MALE; PYRROLIDINES; RATS; RECEPTOR, MELANOCORTIN, TYPE 4; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

ANIMALIA; RATTUS;

EID: 37549009542     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.10.115     Document Type: Article

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