Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands

Authors :: Lars Stank
Annika Frank
Stefanie Hagenow
Holger Stark
Source :: MedChemComm. 10:1926-1929
Publication Year :: 2019
Publisher :: Royal Society of Chemistry (RSC), 2019.
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.