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ID: ALA1149422
Journal: Bioorg Med Chem Lett
Title: Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
Authors: Chen C, Stearns B, Hu T, Anker N, Santini A, Arruda JM, Campbell BT, Datta P, Aiyar J, Munoz B.
Abstract: The SAR of the lead compound 3, a novel ligand for the alpha(2)delta 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.
CiteXplore: 16321528