2-(4-Alkylpiperazin-1-yl)quinolines as a New Class of Imidazole-Free Histamine H₃Receptor Antagonists

Abstract

With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, a series of 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation of the substituents led to highly potent histamine H(3) antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.