SYNTHESIS AND SQAR OF DEQUALINIUM ANALOGS AS K+ CHANNEL BLOCKERS - INVESTIGATIONS ON THE ROLE OF THE 4-AMINO GROUP

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