Talipexole variations as novel bitopic dopamine D 2 and D 3 receptor ligands

Abstract

We linked 5,6,7,8-tetrahydro-4 H -thiazoloazepine scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands.

We linked 2-aminothiazoloazepane scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. Highest D 2 R/D 3 R binding affinities up to p K i 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-4 H -thiazoloazepine derivatives.

We linked 5,6,7,8-tetrahydro-4 H -thiazoloazepine scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands.

We linked 2-aminothiazoloazepane scaffolds with phenylpiperazine pharmacophores to generate bitopic dopamine receptor ligands. Highest D 2 R/D 3 R binding affinities up to p K i 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-4 H -thiazoloazepine derivatives.