Journal of Medicinal Chemistry 2004-05-20

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

Index: J. Med. Chem. 47 , 2833-2838, (2004)

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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.