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ID: ALA3112397

Journal: Bioorg Med Chem Lett

Title: Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives.

Authors: Usuki T, Sato M, Hara S, Yoshimoto Y, Kondo R, Zimmermann S, Kaiser M, Brun R, Hamburger M, Adams M.

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.

CiteXplore: 24433861

DOI: 10.1016/j.bmcl.2013.12.099