Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides are potent antagonists of the human H3-receptor

Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides have been found to be antagonists on the human histamine-3-receptor, showing a Ki value of as low as 4 nM.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (12), p.3162-3165
Hauptverfasser:	PESCHKE, Bernd, BAK, Sonja, HOHLWEG, Rolf, NIELSEN, Rita, VIUFF, Dorthe, RIMVALL, Karin
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Benzene - chemistry Biological and medical sciences Furans - chemistry 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 - metabolism Structure-Activity Relationship Thiophenes - chemistry
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Beschreibung
Zusammenfassung:	Benzo[b]thiophene-2-carboxamides and benzo[b]furan-2-carboxamides have been found to be antagonists on the human histamine-3-receptor, showing a Ki value of as low as 4 nM.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.03.074