The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists

Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-09, Vol.46 (19), p.3957-3960
Hauptverfasser:	Jablonowski, Jill A, Grice, Cheryl A, Chai, Wenying, Dvorak, Curt A, Venable, Jennifer D, Kwok, Annette K, Ly, Kiev S, Wei, Jianmei, Baker, Sherry M, Desai, Pragnya J, Jiang, Wen, Wilson, Sandy J, Thurmond, Robin L, Karlsson, Lars, Edwards, James P, Lovenberg, Timothy W, Carruthers, Nicholas I
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cell Line Dose-Response Relationship, Drug Histamine Antagonists - chemistry Histamine Antagonists - metabolism Histamine Antagonists - pharmacology Humans Indoles - chemistry Indoles - metabolism Indoles - pharmacology Kinetics Ligands Medical sciences Miscellaneous Neurons - cytology Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Radioligand Assay Rats Receptors, Cell Surface - drug effects Receptors, Cell Surface - genetics Receptors, Cell Surface - metabolism Receptors, G-Protein-Coupled Receptors, Histamine Receptors, Histamine H4 Recombinant Proteins - drug effects Recombinant Proteins - genetics Recombinant Proteins - metabolism Structure-Activity Relationship Transfection
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Beschreibung
Zusammenfassung:	Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10 l, which are the first potent and selective histamine H4 receptor antagonists to be described.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm0341047