Issue 11, 2019
From the journal:

MedChemComm

Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands

Lars Stank,a   Annika Frank,a   Stefanie Hagenowa  and  Holger Stark ORCID logo *a  

* Corresponding authors

a Institute of Pharmaceutical and Medicinal Chemistry, Heinrich Heine University Düsseldorf, Universitaetsstr. 1, 40225 Duesseldorf, Germany
E-mail: stark@hhu.de

Abstract

We linked 2-aminothiazoloazepane scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. Highest D2R/D3R binding affinities up to pKi values of 7.74 were observed for compounds containing a 1-(2,3-dichlorophenyl)piperazinoyl moiety, maintaining affinity with deaminated 5,6,7,8-tetrahydro-4H-thiazoloazepine derivatives.

Graphical abstract: Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands

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Article information

DOI
https://doi.org/10.1039/C9MD00379G
Article type
Research Article
Submitted
24 Jul 2019
Accepted
12 Aug 2019
First published
27 Aug 2019

Med. Chem. Commun., 2019,10, 1926-1929

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Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands

L. Stank, A. Frank, S. Hagenow and H. Stark, Med. Chem. Commun., 2019, 10, 1926 DOI: 10.1039/C9MD00379G

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