2. Academic Validation
  3. Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands

Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands

  • Bioorg Med Chem. 2009 Apr 15;17(8):3037-42. doi: 10.1016/j.bmc.2009.03.014.
Dorota Łazewska 1,  Kamil Kuder,  Xavier Ligneau,  Jean-Claude Camelin,  Walter Schunack,  Holger Stark,  Katarzyna Kieć-Kononowicz
Affiliations

Affiliation

  • 1 Jagiellonian University Medical College, Faculty of Pharmacy, Department of Technology and Biotechnology of Drugs, Medyczna 9, 30-688 Kraków, Poland.
PMID: 19329325 DOI: 10.1016/j.bmc.2009.03.014
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).

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