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Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands

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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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Publication details

The article was received on 24 Jul 2019, accepted on 12 Aug 2019 and first published on 27 Aug 2019


Article type: Research Article
DOI: 10.1039/C9MD00379G
Med. Chem. Commun., 2019, Advance Article

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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, Advance Article , DOI: 10.1039/C9MD00379G

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