Novel small molecule bradykinin B sub(1) receptor antagonists. Part 3: Hydroxyurea derivatives

Novel small molecule bradykinin B sub(1) receptor antagonists. Part 3: Hydroxyurea derivatives

Hydroxy urea moieties are introduced as a new class of bradykinin B sub(1) receptor antagonists. First, the SAR of the lead compound was systematically explored. Subsequent optimization resulted in the identification of several biaryl-based hydroxyurea bradykinin B sub(1) receptor antagonists with l...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (3), p.1233-1236
Hauptverfasser: Schnatbaum, Karsten, Schaudt, Marco, Stragies, Roland, Pfeifer, Jochen R, Gibson, Christoph, Locardi, Elsa, Scharn, Dirk, Richter, Uwe, Kalkhof, Holger, Dinkel, Klaus, Zischinsky, Gunther
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Sprache:eng
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Zusammenfassung:Hydroxy urea moieties are introduced as a new class of bradykinin B sub(1) receptor antagonists. First, the SAR of the lead compound was systematically explored. Subsequent optimization resulted in the identification of several biaryl-based hydroxyurea bradykinin B sub(1) receptor antagonists with low-nanomolar activity and very high oral bioavailability in the rat.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2009.11.121