Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 17, 2009, Pages 5195-5199

  Du, Wu ^a   Jewell, James P ^a   Lin, Linus S ^a   Colandrea, Vincent J ^a   Xiao, Jing C ^a   Lao, Julie ^a   Shen, Chun Pyn ^a   Bateman, Thomas J ^a   Reddy, Vijay B G ^a   Ha, Sookhee N ^a   Shah, Shrenik K ^a   Fong, Tung M ^a   Hale, Jeffrey J ^a   Hagmann, William K ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

CB1R; Inverse agonist; Metabolism; Obesity; Synthesis

Indexed keywords

4 (1,1 DIMETHYLHEPTYL) 1',2',3',4',5',6' HEXAHYDRO 2,3' DIHYDROXY 6' (3 HYDROXYPROPYL)BIPHENYL; CANNABINOID 1 RECEPTOR; CANNABINOID 1 RECEPTOR AGONIST; CANNABINOID 1 RECEPTOR INVERSE AGONIST; N [3 (4 CHLOROPHENYL) 2 (3 CYANOPHENYL) 1 METHYLPROPYL] 2 METHYL 2 AMINOPROPANAMIDE; TARANABANT; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CHO CELL; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG BINDING SITE; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; IC 50; MOLECULAR MODEL; NONHUMAN; REACTION ANALYSIS; RECEPTOR AFFINITY; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; ANTI-OBESITY AGENTS; BINDING SITES; COMPUTER SIMULATION; DRUG INVERSE AGONISM; HUMANS; MICROSOMES, LIVER; PYRIDINES; RATS; RECEPTOR, CANNABINOID, CB1; RECEPTOR, CANNABINOID, CB2; RECOMBINANT PROTEINS;

EID: 68349135138     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.07.046     Document Type: Article

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