Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors

Bioorganic and Medicinal Chemistry

Volumn 15, Issue 17, 2007, Pages 5912-5949

  Powell, Noel A ^a   Ciske, Fred L ^a   Cai, Cuiman ^a   Holsworth, Daniel D ^a   Mennen, Ken ^a   Van Huis, Chad A ^a   Jalaie, Mehran ^a   Day, Jacqueline ^a   Mastronardi, Michelle ^a   McConnell, Pat ^a   Mochalkin, Igor ^a   Zhang, Erli ^a   Ryan, Michael J ^a   Bryant, John ^a   Collard, Wendy ^a   Ferreira, Suzie ^a   Gu, Chungang ^a   Collins, Roxane ^a   Edmunds, Jeremy J ^a  

^a PFIZER INC   (United States)

Author keywords

Hypertension; Oral bioavailability; Renin; Structure based drug design

Indexed keywords

6 (2,4 DIAMINO 6 ETHYLPYRIMIDIN 5 YL) 2 (3,5 DIFLUOROPHENYL) 4 (3 METHOXYPROPYL) 2 METHYL 4H BENZO[1,4]OXAZIN 3 ONE; 6 (2,4 DIAMINOPYRIMIDINYL) 1,4 BENZOXAZIN 3 ONE; ALISKIREN; CI 992; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; N [2 [6 (2,4 DIAMINO 6 ETHYLPYRIMIDIN 5 YL) 2 (3,5 DIFLUOROPHENYL) 2 METHYL 3 OXO 2,3 DIHYDROBENZO[1,4]OXAZIN 4 YL]ETHYL]ACETAMIDE; N [2 [6 (2,4 DIAMINO 6 ETHYLPYRIMIDIN 5 YL) 2 METHYL 3 OXO 2 (2,5 DIFLUOROPHENYL) 2,3 DIHYDROBENZO[1,4] OXAZIN 4 YL]ETHYL]ACETAMIDE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; RENIN; RENIN INHIBITOR; TEKTURNA; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CRYSTAL STRUCTURE; DISTRIBUTION VOLUME; DRUG BINDING SITE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; IC 50; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

AMINATION; ANIMALS; BENZOXAZINES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; MALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRIDINES; RATS; RATS, SPRAGUE-DAWLEY; RENIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 34447293062     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2007.05.069     Document Type: Article

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