Moving out of CF -Land: Synthesis, Receptor Affinity, and in silico Studies of NK1 Receptor Ligands Containing a Pentafluorosulfanyl (SF ) Group.

The NK1 receptor (NK1R) is a molecular target for both approved and experimental drugs intended for a variety of conditions, including emesis, pain, and cancers. While contemplating modifications to the typical NK1R pharmacophore, we wondered whether the CF groups common for many NK1R ligands, could be replaced with some other moiety. Our attention was drawn by the SF group, and so we designed, synthesized, and tested ten novel SF -containing compounds for NK1R affinity.