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.
MeSH terms
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Calcium Channels / chemistry
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Calcium Channels / drug effects
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Calcium Channels / metabolism*
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Combinatorial Chemistry Techniques / methods*
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Humans
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Ion Channel Gating*
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Ligands
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Protein Subunits / chemistry
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Protein Subunits / metabolism*
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Solutions / chemistry
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Structure-Activity Relationship
Substances
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Calcium Channels
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Ligands
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Protein Subunits
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Solutions
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voltage gated calcium channel subunit Ca alpha2delta-1, human