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.
Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/15734064113096660050 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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