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

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

Volume: 10 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Kuder J. Kamil, Stachnik Marta, Schunack Walter, Szymanska Ewa and Kiec-Kononowicz Katarzyna, Discovery of Novel Lead in the Group of N-substituted Piperazine Ether Derivatives with Potential Histamine H₃ Receptor Activity, Medicinal Chemistry 2014; 10 (6) . https://dx.doi.org/10.2174/15734064113096660050