ChemMedChem
ChemMedChem
4 years ago

C2-modified Sparteine derivatives are a new class of potentially long-acting Na channel blockers

Hannes Todt, Olaf Scheel, Svilen Simeonov, Ulla Hochenegg, Thomas Knott, John Kudolo, Martina Drescher, Alexander Roller, Nuno Maulide, Vaibhavkumar S. Gawali
The lupin alkaloid Sparteine is a well-known chiral diamine with a range of applications in asymmetric synthesis, as well as a blocker of voltage-gated Na channels (VGSCs). However, there is only scarce information on the VGSC-blocking activity of Sparteine derivatives where the structure of the parent alkaloid is retained. Herein, building on the recent renewed availability of Sparteine and derivatives we report how modification of Sparteine in position 2 produces irreversible blockers of VGSCs. These compounds could be clinically envisaged as long-lasting local anesthetics.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700568

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