合成菜蓟苦素衍生物的抗锥虫结构-活性关系研究
Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives.
作者信息
Usuki Toyonobu, Sato Makiko, Hara Shihori, Yoshimoto Yukiko, Kondo Ryosuke, Zimmermann Stefanie, Kaiser Marcel, Brun Reto, Hamburger Matthias, Adams Michael
机构信息
Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):794-8. doi: 10.1016/j.bmcl.2013.12.099. Epub 2014 Jan 2.
Cynaropicrin is a guaianolide sesquiterpene lactone with a 5-7-5 tricyclic skeleton, four exo-olefins, and two hydroxyl groups. Recently, it was found that the compound is a potent in vitro and in vivo inhibitor of the protozoan parasite Trypanosoma brucei, which causes human African trypanosomiasis (HAT; sleeping sickness). In this Letter, chemical derivatization of cynaropicrin and the structure-activity-relationship (SAR) study against T. brucei is described.
刺菜素是一种愈创木烷型倍半萜内酯，具有5-7-5三环骨架、四个外环烯烃和两个羟基。最近，人们发现该化合物在体外和体内都是原生动物寄生虫布氏锥虫的有效抑制剂，布氏锥虫可导致人类非洲锥虫病（昏睡病）。在这封信中，描述了刺菜素的化学衍生化以及针对布氏锥虫的构效关系（SAR）研究。
Zotero 插件