Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
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).
Łazewska
Dorota
D
Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Kraków, Poland.
Kuder
Kamil
K
Ligneau
Xavier
X
Camelin
Jean-Claude
JC
Schunack
Walter
W
Stark
Holger
H
Kieć-Kononowicz
Katarzyna
K