Discovery of Novel Lead in the Group of N-substituted Piperazine Ether Derivatives with Potential Histamine H-3 Receptor Activity

作者：Kuder Kamil J; Stachnik Marta; Schunack Walter; Szymanska Ewa; Kiec Kononowicz Katarzyna^*

来源：Medicinal Chemistry, 2014, 10(6): 588-599.

DOI：10.2174/15734064113096660050

• Acylpiperazine
• histamine H3R affinity
• histamine H4R affinity
• molecular docking
• non-imidazole histamine H3R ligands

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 H-3 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.

• 出版日期2014