Expedited SAR study of high-affinity ligands to the α2δ subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology

The SAR of the lead compound 3, a novel ligand for the α2δ subunit of voltage-gated calcium channels, was rapidly explored. Utilizing a parallel solution-phase Sn2Ar coupling approach, a focused library was obtained. The library was evaluated in vitro and afforded a series of analogues with improved potencies. The SAR trends of the library are also described.

Figure optionsDownload as PowerPoint slide