Division of Environmental Materials Science, Graduate School of Environmental Science, Hokkaido University, Sapporo 060-0810, Japan.
Sustainable System Research Laboratory, Central Research Institute of Electric Power Industry, Abiko 270-1194, Japan.
Mar Drugs. 2022 Feb 4;20(2):124. doi: 10.3390/md20020124.
Some derivatives of dolastatin 16, a depsipeptide natural product first obtained from the sea hare , were synthesized through second-generation synthesis of two unusual amino acids, dolaphenvaline and dolamethylleuine. The second-generation synthesis enabled derivatizations such as functionalization of the aromatic ring in dolaphenvaline. The derivatives of fragments and whole structures were evaluated for antifouling activity against the cypris larvae of Small fragments inhibited the settlement of the cypris larvae at potent to moderate concentrations (EC = 0.60-4.62 μg/mL), although dolastatin 16 with a substituent on the aromatic ring () was much less potent than dolastatin 16.
一些多拉菌素 16 的衍生物，一种从海螺中首次获得的肽类天然产物，通过两种不寻常的氨基酸，即多拉酚缬氨酸和多拉甲基亮氨酸的第二代合成方法合成。第二代合成使多拉酚缬氨酸的芳环官能化等衍生化成为可能。对这些片段和整个结构的衍生物进行了抗污活性评估，结果表明，小分子片段在有效至中等浓度（EC=0.60-4.62μg/ml）下抑制了幼体的附着，尽管带有芳环取代基的多拉菌素 16（）的活性远低于多拉菌素 16。
