Medicinal Chemistry

Dimitra Hadjipavlou-Litina
Aristotle University of Thessaloniki
Thessaloniki
Greece

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Discovery of Novel Lead in the Group of N-substituted Piperazine Ether Derivatives with Potential Histamine H3 Receptor Activity

Author(s): Kamil J. Kuder, Marta Stachnik, Walter Schunack, Ewa Szymanska, Katarzyna Kiec-Kononowicz.

Graphical Abstract:


Abstract:

The search for novel lead from the group of various substituted N-piperazine ether derivatives was performed. Acyl- and pyridylpiperazine ethyl/propyl ethers were obtained via three different synthetic pathways. Affinity to histamine H3 receptor was established, as well as, for selected compounds, selectivity towards histamine H4R. Docking studies to the histamine H3R homology model strengthened the position of (4-(3-(4-(3-chlorobenzoyl)piperazin-1- yl)propoxy)phenyl)(cyclopropyl)methanone (compound 26) as a novel lead for further studies on histamine H3 receptor antagonist/inverse agonist.

Keywords: Acylpiperazine, histamine H3R affinity, histamine H4R affinity, molecular docking, non-imidazole histamine H3R ligands.

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Article Details

VOLUME: 10
ISSUE: 6
Year: 2014
Page: [588 - 599]
Pages: 12
DOI: 10.2174/15734064113096660050
Price: $58