Tricyclic aminopyrimidine histamine H sub(4 receptor antagonists)
This report discloses the development of a series of tricyclic histamine H sub(4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and wate...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6577-6581 |
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Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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Zusammenfassung: | This report discloses the development of a series of tricyclic histamine H sub(4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H) sub(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model. |
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ISSN: | 0960-894X |
DOI: | 10.1016/j.bmcl.2011.08.014 |