Ureas with histamine H3-antagonist receptor activity : A new scaffold discovered by lead-hopping from cinnamic acid amides

A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5303-5308
Hauptverfasser:	LAU, Jesper F, JEPPESEN, Claus Bekker, RIMVALL, Karin, HOHLWEG, Rolf
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Cinnamates - chemistry ERG1 Potassium Channel Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Histamine Antagonists - chemical synthesis Histamine Antagonists - chemistry Histamine Antagonists - pharmacology Humans Medical sciences Miscellaneous Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Receptors, Histamine H3 - drug effects Stereoisomerism Structure-Activity Relationship Thiazines - chemical synthesis Thiazines - chemistry Thiazines - pharmacology Urea - analogs & derivatives Urea - chemical synthesis Urea - chemistry Urea - pharmacology
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Beschreibung
Zusammenfassung:	A group of tri and tetrasubstituted urea derivatives have been found to be hH(3)-antagonists. The most potent compounds were found in the class of (piperazine-1-yl)-(piperidine-1-yl)-methanones which in addition showed negligible hERG inhibition.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.07.093