Department of Chemistry, Keio University, Yokohama, Kanagawa 223-8522, Japan.
J Org Chem. 2023 Aug 4;88(15):10565-10573. doi: 10.1021/acs.joc.3c00595. Epub 2023 Jul 17.
Ikoamide () is a highly N-methylated antimalarial lipopeptide that was isolated from a marine cyanobacterium, an sp. in 2018, which shows strong antimalarial activity without cytotoxicity against human cancer cell lines. To establish a synthetic method for obtaining enough ikoamide for its biological evaluations, we have established a total synthesis of ikoamide. The synthetic method presented here lays the foundation for the development of novel ikoamide analogues, which may lead to a discovery of pharmaceutically unique antimalarial drug leads.
异寇胺（Ikoamide）是一种高度 N-甲基化的抗疟脂肽，于 2018 年从海洋蓝细菌中分离得到，对人类癌细胞系无细胞毒性，但具有很强的抗疟活性。为建立一种获得足够异寇胺进行生物评价的合成方法，我们已经建立了异寇胺的全合成。这里提出的合成方法为开发新型异寇胺类似物奠定了基础，这可能会发现具有独特药用价值的抗疟药物先导化合物。
