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
Bioorganic & Medicinal Chemistry Letters(2006)
Abstract
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.
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Key words
voltage gated calcium channel
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