Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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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 and Katarzyna Kiec-Kononowicz

Affiliation: Department of Technology and Biotechnology of Drugs, Jagiellonian University, Medical College, Krakow, 30-688, Poland.

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

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.

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Article Details

VOLUME: 10
ISSUE: 6
Page: [588 - 599]
Pages: 12
DOI: 10.2174/15734064113096660050