Exploration of the amine terminus in a novel series of 1,2,4-Triazolo-3-yl- azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists

Article abstract of DOI:10.1021/jm100832d

A novel series of 1,2,4-triazol-3-yl-azabicyclo[3.1.0]hexanes with high affinity and selectivity for the DA D₃ receptor and excellent pharmacokinetic profiles was recently reported. We also recently discussed the role of the linker associated with the triazole moiety. In this manuscript, we are reporting a detailed exploration of the region of the receptor interacting with the amine terminus of the scaffold wherein SAR and developability data associated with these novel templates was undertaken.