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Issue 7, 2015
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Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties†

Paweł Zajdel,*a   Vittorio Canale,a   Anna Partyka,b   Krzysztof Marciniec,c   Rafał Kurczab,d   Grzegorz Satała,d   Agata Siwek,e   Magdalena Jastrzębska-Więsek,b   Anna Wesołowska,b   Tomasz Kos,f   Piotr Popikf  and  Andrzej J. Bojarskid  
Author affiliations

* Corresponding authors

a Department of Medicinal Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland
E-mail: pawel.zajdel@uj.edu.pl
Fax: +48 126205405
Tel: +48 126205450

b Department of Clinical Pharmacy, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland

c Department of Organic Chemistry, Medical University of Silesia, 4 Jagiellońska Street, 41-200 Sosnowiec, Poland

d Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland

e Department of Pharmacobiology, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Krakow, Poland

f Department of Behavioral Neuroscience and Drug Development, Institute of Pharmacology, Polish Academy of Sciences, 12 Smętna Street, 31-343 Kraków, Poland

Abstract

A series of alkyl/arylsulfonamide derivatives of (aryloxy)ethylpiperidines as highly potent 5-HT7 receptor antagonists has been developed through structure-based design on the previously identified compound PZ-766. This resulted in highly potent antagonist10 (3-fluoro-N-(1-{2-[(propan-2-yl)phenoxy]ethyl}piperidin-4-yl)-benzenesulfonamide) which was more active in vivo than PZ-766 and SB-269970 in forced swim test in mice (MED = 2.5 mg kg−1), and displayed comparable effects to SB-269970 in four-plate test in mice (MED = 1.25 mg kg−1) and novel object recognition test in rats (MED = 1 mg kg−1). The results highlight the antidepressant, anxiolytic and pro-cognitive potential of the arylsulfonamide derivatives of (aryloxy)ethylpiperidines with 5-HT7 receptor antagonist properties and warrant further studies to explore their therapeutic potential for the treatment of CNS disorders.

Graphical abstract: Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

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Article information

https://doi.org/10.1039/C5MD00166H
Submitted
21 Apr 2015
Accepted
18 May 2015
First published
19 May 2015
Med. Chem. Commun., 2015,6, 1272-1277
Article type
Concise Article
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Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7 receptor antagonists and their psychotropic properties

P. Zajdel, V. Canale, A. Partyka, K. Marciniec, R. Kurczab, G. Satała, A. Siwek, M. Jastrzębska-Więsek, A. Wesołowska, T. Kos, P. Popik and A. J. Bojarski, Med. Chem. Commun., 2015, 6, 1272
DOI: 10.1039/C5MD00166H

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