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.
Lau
Jesper F
JF
Medicinal Chemistry Research, Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark. jrla@novonordisk.com
Jeppesen
Claus Bekker
CB
Rimvall
Karin
K
Hohlweg
Rolf
R
D002934:Cinnamates / Q000737:chemistry*; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors; D006633:Histamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D002934:Cinnamates; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; D006633:Histamine Antagonists; C000606913:KCNH2 protein, human; D018100:Receptors, Histamine H3; D013843:Thiazines; D014508:Urea