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■ The Synthesis of Simplified Analogues of Crambescin B Carboxylic Acid and Their Inhibitory Activity of Voltage-Gated Sodium Channels: New Aspects of Structure–Activity Relationships

Atsuo Nakazaki,* Shunsuke Mouri, Yoshiki Nakane, Yuki Ishikawa, Mari Yotsu-Yamashita, and Toshio Nishikawa

*Faculty of Science and Engineering, Iwate University, Ueda, Morioka 020-8551 (Japan)

Abstract

We describe the synthesis of six new analogues of crambescin B carboxylic acid from L-aspartic acid and the elucidation of their structure-activity relationships by a cell-based colorimetric assay. All the synthesized analogues except for the C4-analogue were found to have inhibitory activities against voltage-gated sodium channels (VGSCs) in nM order in a cell-based colorimetric assay.