Ion channels play important roles in biological processes and their dysfunction causes lots of diseases including cystic fibrosis. As potential treatment to these channelopathies, synthetic ion channels are being intensively studied. Our group previously reported a small molecule synthetic ion channel utilizing a-aminoxy acids to facilitate chloride transport through lipid bilayer and cell membrane, which can also change membrane voltage and restore chloride conductance in human cystic fibrosis epithelial cells. Here we report the design, synthesis and characterization of ion transporting activities of a series of new analogs with a-amino acids as building blocks. Most of them show high chloride transporting activity, and notably, some can also transport bicarbonate. Transepithelial short circuit current (Isc) measurements using the Ussing chamber setup on calu-3 cell lines have been performed and preliminary positive current response has been observed.

Design, synthesis, characterization, and biological study of potential ion channel compounds

245th National Meeting (2013)

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