Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists

Journal of Medicinal Chemistry

Volumn 54, Issue 24, 2011, Pages 8616-8631

  Hasui, Tomoaki ^a   Matsunaga, Nobuyuki ^a   Ora, Taiichi ^a   Ohyabu, Norio ^a   Nishigaki, Nobuhiro ^a   Imura, Yoshimi ^a   Igata, Yumiko ^a   Matsui, Hideki ^a   Motoyaji, Takashi ^a   Tanaka, Toshimasa ^a   Habuka, Noriyuki ^a   Sogabe, Satoshi ^a   Ono, Midori ^a   Siedem, Christopher S ^b   Tang, Tony P ^b   Gauthier, Cassandra ^b   De Meese, Lisa A ^b   Boyd, Steven A ^b   Fukumoto, Shoji ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b ARRAY BIOPHARMA INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 AMINO 1H IMIDAZOLE 2 THIOL; 2 (BENZYLTHIO)IMIDAZO[2,1 B][1,3,4]THIADIAZOLE; 6 (2 BROMO 2 PHENYLPROPANOYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (2 BROMO 3 PHENYLPROPANOYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (2 BROMOPENTANOYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (2 PHENYL 2H IMIDAZO[2,1 B][1,3,4]THIADIAZIN 3 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (2 PHENYLPROPANOYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (3 PHENYLPROPANOYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (7 BENZYL 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (7 METHYL 7 PHENYL 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (7 PHENYL 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (7 PROPYL 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (BROMOACETYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 (PHENYLACETYL) 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [(2 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [(3 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [(4 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [1 (4 FLUORO 2 METHYLPHENYL) 3 (TRIFLUOROMETHYL) 1H PYRAZOL 5 YL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [7 (2 FLUOROPHENYL) 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [7 (3 FLUOROPHENYL) 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [7 (4 FLUOROPHENYL) 7H [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZIN 6 YL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [BROMO(2 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [BROMO(3 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [BROMO(4 FLUOROPHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 [BROMO(PHENYL)ACETYL] 2H 1,4 BENZOXAZIN 3 (4H)ONE; 6 PENTANOYL 2H 1,4 BENZOXAZIN 3 (4H)ONE; BENZOXAZIN 3 ONE DERIVATIVE; MINERALOCORTICOID ANTAGONIST; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIHYPERTENSIVE ACTIVITY; ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH THROUGHPUT SCREENING; MOLECULAR DOCKING; NONHUMAN; RAT;

ANIMALS; ANTIHYPERTENSIVE AGENTS; BENZOXAZINES; BINDING, COMPETITIVE; CRYSTALLOGRAPHY, X-RAY; MICROSOMES, LIVER; MODELS, MOLECULAR; PROTEIN CONFORMATION; PYRAZOLES; RATS; RATS, WISTAR; RECEPTORS, MINERALOCORTICOID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84055217558     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2011645     Document Type: Article

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