Discovery of piperazin-1-ylpyridazine-based potent and selective stearoyl-CoA Desaturase-1 inhibitors for the treatment of obesity and metabolic syndrome

Journal of Medicinal Chemistry

Volumn 56, Issue 2, 2013, Pages 568-583

  Zhang, Zaihui ^a   Sun, Shaoyi ^a   Kodumuru, Vishnumurthy ^a   Hou, Duanjie ^a   Liu, Shifeng ^a   Chakka, Nagasree ^a   Sviridov, Serguei ^a   Chowdhury, Sultan ^a   McLaren, David G ^a   Ratkay, Leslie G ^a   Khakh, Kuldip ^a   Cheng, Xing ^a   Gschwend, Heinz W ^b   Kamboj, Rajender ^a   Fu, Jianmin ^a   Winther, Michael D ^a  

^a Xenon Pharmaceuticals Inc   (Canada)

^b Consultant ^*  (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6 [4 [5 CHLORO 2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]N(2 CYCLOPROPYLETHYL)PYRIDAZINE 3 CARBOXAMIDE; ANTIOBESITY AGENT; N BENZYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N HEPTYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL)PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N HEXYL 5 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIMIDINE 2 CARBOXAMIDE; N HEXYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL)PYRIDAZINE 3 CARBOXAMIDE; N ISOPENTYL 2 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIMIDINE 5 CARBOXAMIDE; N ISOPENTYL 5 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PICOLINAMIDE; N ISOPENTYL 5 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRAZINE 2 CARBOXAMIDE; N ISOPENTYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N PENTYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N PHENETHYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N PHENYL 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 CYCLOPROPYLETHYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 CYCLOPROPYLETHYL) 6 [4 [5 FLUORO 2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 ETHOXYETHYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 HYDROXY 2 PHENYLETHYL) 6 [4 [2 (TRIFLUOROMETHYL)-BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 OXO 2 PHENYLETHYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(2 PHENYLPROPYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(3 CYCLOPROPYLPROPYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(3 HYDROXY 3 METHYLBUTYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(3 PHENYLPROPYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(4 CHLOROPHENYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(4 CYCLOPROPYLBUTYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N(CYCLOPROPYLMETHYL) 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; N[1H BENZO(D)IMIDAZOL 2 YL] 6 [4 [2 (TRIFLUOROMETHYL)BENZOYL]PIPERAZIN 1 YL]PYRIDAZINE 3 CARBOXAMIDE; OXYGENASE INHIBITOR; PIPERAZINE DERIVATIVE; PYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; XEN 103;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN HEPG2; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DOSE COMPARISON; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IC 50; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; METABOLIC SYNDROME X; MOUSE; NONHUMAN; OBESITY; RAT; STRUCTURE ACTIVITY RELATION; WEIGHT GAIN;

ANIMALS; ENZYME INHIBITORS; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; METABOLIC SYNDROME X; MICE; OBESITY; PIPERAZINES; PYRIDAZINES; RATS; RATS, ZUCKER; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STEAROYL-COA DESATURASE;

EID: 84872804303     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301661h     Document Type: Article

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