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Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands
Lars Stank,Annika Frank,Stefanie Hagenow,Holger Stark
MedChemComm Pub Date : 08/27/2019 00:00:00 , DOI:10.1039/C9MD00379G
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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