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
Hauptverfasser: Savall, Brad M, Gomez, Laurent, Chavez, Frank, Curtis, Michael, Meduna, Steven P, Kearney, Aaron, Dunford, Paul, Cowden, Jeffery, Thurmond, Robin L, Grice, Cheryl, Edwards, James P
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Sprache:eng
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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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2011.08.014