Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: Effects of substitution about the rigidifying ring

Three novel series of histamine H(4) receptor (H(4)R) antagonists containing the 2-aminopyrimidine motif are reported. The best of these compounds display good in vitro potency in both functional and binding assays. In addition, representative compounds are able to completely block itch responses wh...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (6), p.1900-1904
Hauptverfasser:	KOENIG, John R, HUAQING LIU, BRIONI, Jorge D, COWART, Marlon, DRIZIN, Irene, WITTE, David G, CARR, Tracy L, MANELLI, Arlene M, MILICIC, Ivan, STRAKHOVA, Marina I, MILLER, Thomas R, ESBENSHADE, Timothy A
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminopyridines - pharmacology Animals Biological and medical sciences Histamine and antagonists. Allergy Histamine Antagonists - pharmacology Humans Medical sciences Mice Pharmacology. Drug treatments Receptors, G-Protein-Coupled - antagonists & inhibitors Receptors, Histamine Receptors, Histamine H4
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Zusammenfassung:	Three novel series of histamine H(4) receptor (H(4)R) antagonists containing the 2-aminopyrimidine motif are reported. The best of these compounds display good in vitro potency in both functional and binding assays. In addition, representative compounds are able to completely block itch responses when dosed ip in a mouse model of H(4)-agonist induced scratching, thus demonstrating their activities as H(4)R antagonists.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.01.131