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.
Peschke
Bernd
B
Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Maaloev, Denmark. bpes@novonordisk.com
Bak
Sonja
S
Hohlweg
Rolf
R
Nielsen
Rita
R
Viuff
Dorthe
D
Rimvall
Karin
K
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001554:Benzene / Q000737:chemistry; D005663:Furans / Q000737:chemistry*; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry*
D000577:Amides; D005663:Furans; D006633:Histamine Antagonists; D018100:Receptors, Histamine H3; D013876:Thiophenes; D001554:Benzene; C039281:furan