Discovery of morpholine-based aryl sulfonamides as Na v 1.7 inhibitors
2018
Abstract Replacement of the
piperidinering in the lead benzenesulfonamide Na v 1.7 inhibitor 1 with a weakly basic
morpholinecore resulted in a significant reduction in Na v 1.7 inhibitory activity, but the activity was restored by shortening the linkage from methyleneoxy to oxygen. These efforts led to a series of
morpholine-based aryl sulfonamides as isoform-selective Na v 1.7 inhibitors. This report describes the synthesis and SAR of these analogs.
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