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Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands |
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| Authors: | Dorota ?a?ewska Kamil Kuder Xavier Ligneau Jean-Claude Camelin Walter Schunack Holger Stark Katarzyna Kie?-Kononowicz |
| Institution: | 1. Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Kraków, Poland;2. Bioprojet-Biotech, 4 rue du Chesnay Beauregard, BP 96205, 35762 Saint-Grégoire, France;3. Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Strasse 2+4, 14195 Berlin, Germany;4. Institut für Pharmazeutische Chemie, Biozentrum, ZAFES/LiFF/CMP, Johann Wolfgang Goethe-Universität, Max-von-Laue-Strasse 9, 60438 Frankfurt/Main, Germany |
| Abstract: | Synthesis and biological activities of a series of homo- or substituted piperidine unsymmetrical diethers are described. The novel compounds were evaluated for histamine H3 receptor binding affinities at recombinant human H3 receptor stably expressed in HEK-293 cells. All diethers showed in vitro affinities in nanomolar concentration range. The most potent compounds are 1-3-(3-(4-chlorophenoxy)propoxy)propyl]-3-methylpiperidine 11 (Ki = 3.2 nM) and 1-3-(3-(4-chlorophenoxy)propoxy)propyl]azepane 13 (Ki = 3.5 nM). |
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