| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594814 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
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.
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Authors
Toyonobu Usuki, Makiko Sato, Shihori Hara, Yukiko Yoshimoto, Ryosuke Kondo, Stefanie Zimmermann, Marcel Kaiser, Reto Brun, Matthias Hamburger, Michael Adams,