Design, synthesis and biological activity of original pyrazolo-pyrido- diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors

Bioorganic and Medicinal Chemistry

Volumn 19, Issue 23, 2011, Pages 6989-6999

  Gaggini, Francesca ^a   Laleu, Benoît ^a   Orchard, Mike ^a   Fioraso Cartier, Laetitia ^a   Cagnon, Laurne ^a   Houngninou Molango, Sophie ^a   Gradia, Angelo ^a   Duboux, Guillaume ^a   Merlot, Cédric ^a   Heitz, Freddy ^a   Szyndralewiez, Cédric ^a   Page, Patrick ^a  

^a GENKYOTEX SA   (Switzerland)

Author keywords

Antifibrotic; Inhibitor; IPF; NADPH oxidase; Nox1; Nox4; Pirfenidone; Pyrazolo pyrido dione

Indexed keywords

10 (2 CHLOROBENZYL) 2 (2 CHLOROPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 10 (3 CHLOROBENZYL) 2 (2 CHLOROPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 10 (3 METHOXYBENZYL) 2 (2 METHOXYPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 10 (4 CHLOROBENZYL) 2 (2 CHLOROPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 10 BENZYL 2 (2 CHLOROPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 10 BENZYL 2 (2 METHOXYPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 10 (2 METHOXYBENZYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 10 (4 METHOXYBENZYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 10 (FURAN 3 YLMETHYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 10 (PYRIDIN 2 YLMETHYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 10 (PYRIDIN 3 YLMETHYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 CHLOROPHENYL) 2,3,7,8 TETRAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [2,1 C] [1,4] OXAZINE 1,5 (10H) DIONE; 2 (2 CHLOROPHENYL) 2,3,8,9,10,11 HEXAHYDRO 1HPYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 2 (2 METHOXYPHENYL) 10 (PYRIDIN 2 YLMETHYL) 2,3,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 1,5 (7H) DIONE; 9 BENZYL 2 (2 CHLOROPHENYL) 2,3,7,8,9,10 HEXAHYDROPYRAZOLO [4',3':3,4] PYRIDO [1,2 A] PYRAZINE 1,5 DIONE; ANTIFIBROTIC AGENT; DIAZEPINE DERIVATIVE; OXAZINE DERIVATIVE; PIRFENIDONE; PYRAZINE DERIVATIVE; PYRAZOLONE DERIVATIVE; PYRIDONE DERIVATIVE; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE OXIDASE 1; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE OXIDASE 1 INHIBITOR; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE OXIDASE 4; REDUCED NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE OXIDASE 4 INHIBITOR; TERT BUTYL 2 (2 CHLOROPHENYL) 1,5 DIOXO 2,3,5,8,9,10,11 HEXAHYDRO 1H PYRAZOLO [4',3':3,4] PYRIDO [1,2 A] [1,4] DIAZEPINE 10 (7H) CARBOXYLIC ACID; UNCLASSIFIED DRUG;

AMINATION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CELL DIFFERENTIATION; DEPROTECTION REACTION; DISTRIBUTION VOLUME; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME SPECIFICITY; HUMAN; HUMAN CELL; LUNG FIBROBLAST; LUNG FIBROSIS; MALE; MAXIMUM PLASMA CONCENTRATION; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN TARGETING; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; AZEPINES; BLEOMYCIN; DISEASE MODELS, ANIMAL; ENZYME INHIBITORS; HUMANS; MALE; MICE; MICE, INBRED C57BL; NADPH OXIDASE; OXAZINES; PULMONARY FIBROSIS; PYRAZINES; PYRIDONES; STRUCTURE-ACTIVITY RELATIONSHIP;

MURINAE;

EID: 80655136948     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.10.016     Document Type: Article

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