1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H(3) receptor. The most potent amides had antagonist potencies in the subnanomolar range.
Zaragoza
Florencio
F
Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Malov, Denmark. flo@novonordisk.com
Stephensen
Henrik
H
Knudsen
Sanne M
SM
Pridal
Lone
L
Wulff
Birgitte S
BS
Rimvall
Karin
K
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship
D006633:Histamine Antagonists; D010879:Piperazines; D018100:Receptors, Histamine H3