Piperidine variations in search for non-imidazole histamine H3 receptor ligands

Bioorganic & Medicinal Chemistry
2008.0

Abstract

Synthesis and biological evaluation of the novel histamine H(3) receptor ligands is described. Two series of ethers (aliphatic and aromatic) have been prepared by four different methods. Compounds were evaluated for their affinities at recombinant human H(3) receptor stably expressed in CHO cells. The ethers show from low to moderate in vitro affinities in nanomolar concentration range. The most potent compound was the 1-[3-(4-tert-butylphenoxy)propyl]-4-piperidino-piperidine 16 (hH(3)R K(i)=100 nM). Several members of the new series investigated under in vivo conditions, proved to be inactive.

Knowledge Graph

Similar Paper

Piperidine variations in search for non-imidazole histamine H3 receptor ligands
Bioorganic & Medicinal Chemistry 2008.0
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands
European Journal of Medicinal Chemistry 2018.0
Synthesis and biological activity of novel tert -amylphenoxyalkyl (homo)piperidine derivatives as histamine H 3 R ligands
Bioorganic & Medicinal Chemistry 2017.0
Optimization and preclinical evaluation of novel histamine H3receptor ligands: Acetyl and propionyl phenoxyalkyl piperazine derivatives
Bioorganic & Medicinal Chemistry 2018.0
Synthesis and in Vitro Pharmacology of a Series of New Chiral Histamine H<sub>3</sub>-Receptor Ligands:  2-(RandS)-Amino-3-(1H-imidazol-4(5)-yl)propyl Ether Derivatives
Journal of Medicinal Chemistry 1999.0
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands
Bioorganic &amp; Medicinal Chemistry 2017.0
Development of a New Class of Nonimidazole Histamine H<sub>3</sub> Receptor Ligands with Combined Inhibitory Histamine N-Methyltransferase Activity
Journal of Medicinal Chemistry 2002.0
(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands
European Journal of Medicinal Chemistry 2015.0
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists
European Journal of Medicinal Chemistry 2009.0
Synthesis and structure–activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists
Bioorganic &amp; Medicinal Chemistry Letters 2004.0