Synthesis and pharmacological testing of polyaminoquinolines as blockers of the apamin-sensitive Ca 2+-activated K+ channel (SK Ca)

DI Fletcher, CR Ganellin, A Piergentili, PM Dunn…

文献索引：Fletcher, David I.; Ganellin, C. Robin; Piergentili, Alessandro; Dunn, Philip M.; Jenkinson, Donald H. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 16 p. 5457 - 5479

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被引用次数: 8

摘要

The synthesis and pharmacological testing of a series of non-peptidic blockers of the SKCa (SK-3) channel is described. Target compounds were designed to mimic the spatial relationships of selected key residues in the energy-minimised structure of the octadecapeptide apamin, which are a highly potent blocker of this channel. Structures consist of a central unit, either a fumaric acid or an aromatic ring, to which are attached ...