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

被引：16

作者：

Lazewska, Dorota ^{[1
]}

Kuder, Kamil ^{[1
]}

Ligneau, Xavier ^{[2
]}

Schwartz, Jean-Charles ^{[2
]}

Schunack, Walter ^{[3
]}

Stark, Holger ^{[4
]}

Kiec-Kononowicz, Katarzyna ^{[1
]}

机构：

[1] Jagiellonian Univ, Coll Med, Fac Pharm, Dept Technol & Biotechnol Drugs, PL-30688 Krakow, Poland

[2] Bioprojet Biotech, F-35762 St Gregoire, France

[3] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany

[4] Goethe Univ Frankfurt, Biozentrum ZAFES, Inst Pharmazeut Chem, D-60438 Frankfurt, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 18期

关键词：

histamine; H-3; receptor; non-imidazole ligands; piperidine derivatives;

D O I：

10.1016/j.bmc.2008.07.071

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 affiities 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. (C) 2008 Published by Elsevier Ltd.

引用

页码：8729 / 8736

页数：8

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