Takamura Hiroyoshi, Ohashi Takumi, Kikuchi Takahiro, Endo Noriyuki, Fukuda Yuji, Kadota Isao
Department of Chemistry, Graduate School of Natural Science and Technology, Okayama University, 3-1-1 Tsushimanaka, Kita-ku, Okayama 700-8530, Japan.
Org Biomol Chem. 2017 Jul 5;15(26):5549-5555. doi: 10.1039/c7ob01160a.
Hybrid molecules consisting of geraniol and butenolide were designed and synthesized by the late-stage divergent strategy. In the synthetic route, ring-closing metathesis was utilized for the construction of a butenolide moiety. A biological evaluation of the eight synthetic hybrid compounds revealed that these molecules exhibit antifouling activity against the cypris larvae of the barnacle Balanus (Amphibalanus) amphitrite with EC values of 0.30-1.31 μg mL. These results show that hybridization of the geraniol and butenolide structural motifs resulted in the enhancement of the antifouling activity.
通过后期发散策略设计并合成了由香叶醇和丁烯内酯组成的杂化分子。在合成路线中，利用关环复分解反应构建丁烯内酯部分。对这八种合成杂化化合物的生物学评估表明，这些分子对藤壶白脊藤壶（Amphibalanus amphitrite）的金星幼虫具有防污活性，EC值为0.30 - 1.31 μg/mL。这些结果表明，香叶醇和丁烯内酯结构基序的杂化导致了防污活性的增强。
