Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile

A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several members of this compound library were identified as high-affinity dopamine D3 and D2 receptor ligands. The most interesting representative, compound 2, showed potent antipsychotic behaviour coupled with a beneficial cognitive and EPS profile.

Graphical abstractNovel arylsulfonamides were identified as high-affinity dopamine D3 and D2 receptor ligands. Some derivatives were found to be active in antipsychotic tests in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide