Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives

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• 作者：Toyonobu Usuki ; Makiko Sato ; Shihori Hara ; Yukiko Yoshimoto ; Ryosuke Kondo ; Stefanie Zimmermann ; Marcel Kaiser ; Reto Brun ; Matthias Hamburger ; Michael Adams
• 关键词：Cynaropicrin ; Guaianolide ; Trypanosoma brucei ; SAR ; Derivatization
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 February, 2014
• 年：2014
• 卷：24
• 期：3
• 页码：794-798
• 全文大小：357 K

文摘

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.