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Arch Pharm (Weinheim). 2013 Mar;346(3):180-8. doi: 10.1002/ardp.201200322. Epub 2013 Feb 4.

Quinolinesulfonamides of aryloxy-/arylthio-ethyl piperidines: influence of an arylether fragment on 5-HT1A/5-HT7 receptor selectivity.

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1
Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland.

Abstract

The solid-phase synthesis of a new series of 19 biomimetics of long-chain arylpiperazines, namely flexible quinoline sulfonamides of aryl(heteroaryl)oxy-/heteroarylthio-ethyl 4-aminomethylpiperidines, is reported. Various structural modifications applied followed by biological evaluation for 5-HT1A, 5-HT6, and 5-HT7 receptors gave further support of a possible replacement of arylpiperazine with aryloxy-/arylthio-ethyl derivatives of alicyclic amines and control of receptor selectivity upon diversification in the aryl(heteroaryl)oxy-/heteroarylthio-ethyl fragment.

PMID:
23381952
DOI:
10.1002/ardp.201200322
[Indexed for MEDLINE]
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