1-Alkyl-4-acylpiperazines as a New Class of Imidazole-Free Histamine H₃ Receptor Antagonists

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.