SYNTHESIS AND SQAR OF DEQUALINIUM ANALOGS AS K- INVESTIGATIONS ON THEROLE OF THE 4-AMINO GROUP( CHANNEL BLOCKERS )

Dequalinium (1) is a potent and selective non-peptidic blocker of the SKCa channel. The contribution of the 4-amino group to activity was in vestigated by replacing it by other groups R(4). The size or lipophili city of R(4) was found to be unimportant and a good correlation was ob tained between sigma(R) for R(4) and the blocking potency of the analo gues, suggesting that the role of the NH2 group is electronic.