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 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Schnatbaum, Karsten Schaudt, Marco Stragies, Roland Pfeifer, Jochen R Gibson, Christoph Locardi, Elsa Scharn, Dirk Richter, Uwe Kalkhof, Holger Dinkel, Klaus Zischinsky, Gunther |
description | 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. |
doi_str_mv | 10.1016/j.bmcl.2009.11.121 |
format | Article |
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title | Novel small molecule bradykinin B sub(1) receptor antagonists. Part 3: Hydroxyurea derivatives |
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