1. Talipexole variations as novel bitopic dopamine D2 and D3 receptor ligands
- Author
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Lars Stank, Annika Frank, Stefanie Hagenow, and Holger Stark
- Subjects
Pharmacology ,010405 organic chemistry ,Chemistry ,Stereochemistry ,Organic Chemistry ,Pharmaceutical Science ,Phenylpiperazine ,01 natural sciences ,Biochemistry ,Talipexole ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,Dopamine receptor D3 ,Dopamine receptor ,Dopamine receptor D2 ,Drug Discovery ,medicine ,Molecular Medicine ,Moiety ,Pharmacophore ,Binding affinities ,medicine.drug - 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.
- Published
- 2019
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