Antitrypanosomal structure–activity-relationship study of synthetic cynaropicrin derivatives

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-02, Vol.24 (3), p.794-798
Hauptverfasser:	Usuki, Toyonobu, Sato, Makiko, Hara, Shihori, Yoshimoto, Yukiko, Kondo, Ryosuke, Zimmermann, Stefanie, Kaiser, Marcel, Brun, Reto, Hamburger, Matthias, Adams, Michael
Format:	Artikel
Sprache:	eng
Schlagworte:	Cynaropicrin Derivatization Guaianolide Inhibitory Concentration 50 Lactones - chemical synthesis Lactones - chemistry Lactones - pharmacology Molecular Structure SAR Sesquiterpenes - chemical synthesis Sesquiterpenes - chemistry Sesquiterpenes - pharmacology Structure-Activity Relationship Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma brucei Trypanosoma brucei brucei - drug effects
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.12.099