Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SK Ca channels in sympathetic neurons

…, CR Ganellin, JQ Chen, D Gunasekera…

文献索引：Galanakis, Dimitrios; Ganellin, C. Robin; Chen, Jian-Quing; Gunasekera, Diyan; Dunn, Philip M. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4231 - 4235

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被引用次数: 15

摘要

The synthesis, pharmacological evaluation, and molecular modeling studies of unsymmetrical bis-alkylene bis-quinolinium cyclophanes and xylylene–alkylene bis- quinolinium cyclophanes is described. Two important structural features of the pharmacophore for SKCa channel blockade have been identified. These are (i) an optimum distance of ca. 5.8 Å between the centroids of the pyridinium rings of the two quinolinium ...