从海洋蓝细菌中分离得到抗变形虫内酰胺 hoshinolactam 的全合成。
Isolation and Total Synthesis of Hoshinolactam, an Antitrypanosomal Lactam from a Marine Cyanobacterium.
机构信息
Department of Chemistry, Keio University , 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, Kanagawa 223-8522, Japan.
Research Center for Tropical Diseases, Kitasato Institute for Life Sciences, and §Graduate School of Infection Control Sciences, Kitasato University , 5-9-1, Shirokane, Minato-ku, Tokyo 108-8641, Japan.
出版信息
Org Lett. 2017 Feb 17;19(4):890-893. doi: 10.1021/acs.orglett.7b00047. Epub 2017 Feb 1.
In the search for new antiprotozoal substances, hoshinolactam, an antitrypanosomal lactam, was isolated from a marine cyanobacterium. The gross structure was elucidated by spectroscopic analyses, and the absolute configuration was determined by the first total synthesis. Hoshinolactam showed potent antitrypanosomal activity with an IC value of 3.9 nM without cytotoxicity against human fetal lung fibroblast MRC-5 cells (IC > 25 μM).
在寻找新的抗原生动物物质的过程中，从一种海洋蓝细菌中分离得到了抗锥虫内酯 hoshinolactam。通过光谱分析阐明了其总体结构，并通过首次全合成确定了其绝对构型。Hoshinolactam 表现出很强的抗锥虫活性，IC 值为 3.9 nM，对人胎肺成纤维细胞 MRC-5 细胞无细胞毒性（IC > 25 μM）。
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