title: Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
abstract: Synthesis and biological activities of a series of homo- or substituted piperidine unsymmetrical diethers are described. The novel compounds were evaluated for histamine H(3) receptor binding affinities at recombinant human H(3) 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 (K(i)=3.2 nM) and 1-[3-(3-(4-chlorophenoxy)propoxy)propyl]azepane 13 (K(i)=3.5 nM).
authors.affiliation: Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Kraków, Poland.
authors.forename: Dorota
authors.initials: D
authors.lastname: Łazewska
authors.forename: Kamil
authors.initials: K
authors.lastname: Kuder
authors.forename: Xavier
authors.initials: X
authors.lastname: Ligneau
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Camelin
authors.forename: Walter
authors.initials: W
authors.lastname: Schunack
authors.forename: Holger
authors.initials: H
authors.lastname: Stark
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Kieć-Kononowicz