1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists

Florencio Zaragoza; Henrik Stephensen; Sanne M Knudsen; Lone Pridal; Birgitte S Wulff; Karin Rimvall

doi:10.1021/jm031028z

1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists

J Med Chem. 2004 May 20;47(11):2833-8. doi: 10.1021/jm031028z.

Authors

Florencio Zaragoza¹, Henrik Stephensen, Sanne M Knudsen, Lone Pridal, Birgitte S Wulff, Karin Rimvall

Affiliation

¹ Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Malov, Denmark. flo@novonordisk.com

PMID: 15139761
DOI: 10.1021/jm031028z

Abstract

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.

MeSH terms

Animals
CHO Cells
Cricetinae
Histamine Antagonists / chemical synthesis*
Histamine Antagonists / chemistry
Histamine Antagonists / pharmacology
Humans
Piperazines / chemical synthesis*
Piperazines / chemistry
Piperazines / pharmacology
Radioligand Assay
Receptors, Histamine H3 / drug effects*
Structure-Activity Relationship

Substances

Histamine Antagonists
Piperazines
Receptors, Histamine H3