Tricyclic aminopyrimidine histamine H4 receptor antagonists

This report discloses the development of a series of tricyclic histamine H(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 s...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-11, Vol.21 (21), p.6577-6581
Hauptverfasser:	SAVALL, Brad M, GOMEZ, Laurent, EDWARDS, James P, CHAVEZ, Frank, CURTIS, Michael, MEDUNA, Steven P, KEARNEY, Aaron, DUNFORD, Paul, COWDEN, Jeffery, THURMOND, Robin L, GRICE, Cheryl
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Histamine and antagonists. Allergy Histamine Antagonists - chemistry Histamine Antagonists - pharmacology Medical sciences Mice Pharmacology. Drug treatments Receptors, G-Protein-Coupled - antagonists & inhibitors Receptors, Histamine Receptors, Histamine H4
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Beschreibung
Zusammenfassung:	This report discloses the development of a series of tricyclic histamine H(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(4) receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.08.014