Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2- chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist

Bioorganic and Medicinal Chemistry

Volumn 18, Issue 17, 2010, Pages 6377-6388

  Lee, Jinhwa ^a   Seo, Hee Jeong ^a   Lee, Suk Ho ^a   Kim, Jeongmin ^a   Jung, Myung Eun ^a   Lee, Sung Han ^a   Song, Kwang Seop ^a   Lee, Junwon ^a   Kang, Suk Youn ^a   Kim, Min Ju ^a   Kim, Mi Soon ^a   Son, Eun Jung ^a   Lee, Minwoo ^a   Han, Ho Kyun ^a  

^a Green Cross Company   (South Korea)

Author keywords

Cannabinoid; Obesity; Rimonabant; Thiadiazole; Triazole

Indexed keywords

2 (4 ((1H 1,2,4 TRIAZOL 1 YL)METHYL) 5 (4 BROMOPHENYL) 1 (2 CHLOROPHENYL) 1H PYRAZOL 3 YL) 5 TERT BUTYL 1,3,4 THIADIAZOLE; 2 (4 ((1H 1,2,4 TRIAZOL 1 YL)METHYL) 5 (4 BROMOPHENYL) 1 (2,4 DICHLOROPHENYL) 1H PYRAZOL 3 YL) 5 TERT BUTYL 1,3,4 THIADIAZOLE; 2 (4 ((1H 1,2,4 TRIAZOL 1 YL)METHYL) 5 (4 CHLOROPHENYL) 1 (2,4 DICHLOROPHENYL) 1H PYRAZOL 3 YL) 5 (1 (TRIFLUOROMETHYL) CYCLOBUTYL) 1,3,4 THIADIAZOLE; CANNABINOID 1 RECEPTOR ANTAGONIST; GCC 2680; RIMONABANT; TARANABANT; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; RAT; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; HUMANS; MALE; MICE; MICE, INBRED C57BL; OBESITY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, CANNABINOID, CB1; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES;

ANIMALIA;

EID: 77955982624     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.07.013     Document Type: Article

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