Novel small molecule bradykinin B2 receptor antagonists

Journal of Medicinal Chemistry

Volumn 52, Issue 14, 2009, Pages 4370-4379

  Gibson, Christoph ^a   Schnatbaum, Karsten ^a   Pfeifer, Jochen R ^a   Locardi, Elsa ^a   Paschke, Matthias ^a   Reimer, Ulf ^a   Richter, Uwe ^a   Scharn, Dirk ^a   Faussner, Alexander ^b   Tradler, Thomas ^a  

^a Jerini AG   (Germany)

^b UNIVERSITY OF MUNICH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 METHYL 3 [2 METHYL 4 (4 METHYL 2H PYRAZOL 3 YL)QUINOLIN 8 YLOXYMETHYL]PYRIDIN 2 YLMETHYL] 3 TRIFLUOROMETHYL 1H PYRIDIN 2 ONE; ASPARAGINE; BRADYKININ B2 RECEPTOR; BRADYKININ B2 RECEPTOR ANTAGONIST; CYTOCHROME P450; JSM 10292; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ALKYLATION; ANGIONEUROTIC EDEMA; ARTICLE; BINDING AFFINITY; CARBONYLATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; HYDROGEN BOND; LIVER MICROSOME; MOLECULAR WEIGHT; PHARMACOPHORE; SOLUBILITY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CELL LINE; DRUG DESIGN; FEMALE; HETEROCYCLIC COMPOUNDS; HUMANS; MOLECULAR WEIGHT; QUINOLINES; RATS; RATS, WISTAR; RECEPTOR, BRADYKININ B2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 67650723122     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9002445     Document Type: Article

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43. all. A substantial amount of 52e was detected in the last obtained plasma sample (480 min), which means that the actual oral bioavailability is significantly higher than 17%.