Discovery of novel benzoxazinones as potent and orally active long chain fatty acid elongase 6 inhibitors

Journal of Medicinal Chemistry

Volumn 52, Issue 22, 2009, Pages 7289-7300

  Mizutani, Takashi ^a   Ishikawa, Shiho ^a   Nagase, Tsuyoshi ^a   Takahashi, Hidekazu ^a   Fujimura, Takashi ^a   Sasaki, Takahide ^a   Nagumo, Akira ^a   Shimamura, Ken ^a   Miyamoto, Yasuhisa ^a   Kitazawa, Hidefumi ^a   Kanesaka, Maki ^a   Yoshimoto, Ryo ^a   Aragane, Katsumi ^a   Tokita, Shigeru ^a   Sato, Nagaaki ^a  

^a BANYU PHARMACEUTICAL CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

1 [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 3 (4 FLUOROPHENYL)UREA; 4 FLUORO N [[2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[2 OXO 6 (1H PYRAZOL 1 YL) 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[2 OXO 6 (1H PYRAZOL 4 YL) 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[2 OXO 6 (1H PYRAZOL 5 YL) 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[2 OXO 6 [2 OXOPYRIDIN 1(2H) YL] 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[2 OXO 6 PHENYL 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; 4 FLUORO N [[6 (ISOXAZOL 4 YL) 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BENZAMIDE; [6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL (4-FLUOROPHENYL)CARBAMATE; BENZOXAZINONE DERIVATIVE; EFAVIRENZ; ENZYME; ENZYME INHIBITOR; LONG CHAIN FATTY ACID; LONG CHAIN FATTY ACID ELONGASE 6; LONG CHAIN FATTY ACID ELONGASE 6 INHIBITOR; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 2 (4 FLUOROPHENYL)ACETAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 2 FLUOROBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 2 METHYLBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 3 FLUOROBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 3 METHYLBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 (METHYLSULFONYL)BENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 (PROPAN 2 YL)BENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 (TRIFLUOROMETHYL)BENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 FLUOROBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 METHOXYBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL] 4 METHYLBENZAMIDE; N [[6 CHLORO 2 OXO 4 (TRIFLUOROMETHYL) 1,4 DIHYDRO 2H 3,1 BENZOXAZIN 4 YL]METHYL]BIPHENYL 4 CARBOXAMIDE; PYRAZOLE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ACETYLTRANSFERASES; ADMINISTRATION, ORAL; ANIMALS; BENZOXAZINES; CELL LINE, TUMOR; DRUG DISCOVERY; ENZYME INHIBITORS; FATTY ACIDS; HUMANS; LIVER; MALE; MICE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 70949083359     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900915x     Document Type: Article

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