The dopamine receptor type 3 (D3R) is a G-protein-coupled receptor (GPCR) and it is a drug target for multiple neurological and psychiatric disorders such as Parkinson’s disease, schizophrenia and drug addiction. D3R ligands with high affinity and selectivity against other dopamine receptors are highly demanded. Many known ligands have the common pharmacophore with an arylpiperazine linked with an aryl amide. Here we explore the new scaffolds with different site variations. 1), Replacement of the piperazine with various diaza ring systems; 2), employment of the cyclohexane instead of the chain linker; 3), exchange the ary amide with a carbamide (thiocarbamide) or with a 1,2,4-triazole moiety. The design, synthesis of the ligands, their affinities to D3R as well as to D2R and the structure-activity relationships will be presented.

Noval dopamine receptor (D3) ligands with new scaffolds

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.