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Antitrypanosomal structure-activity-relationship study of synthetic cynaropicrin derivatives.
Usuki, Toyonobu; Sato, Makiko; Hara, Shihori; Yoshimoto, Yukiko; Kondo, Ryosuke; Zimmermann, Stefanie; Kaiser, Marcel; Brun, Reto; Hamburger, Matthias; Adams, Michael.
Afiliação
  • Usuki T; Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan. Electronic address: t-usuki@sophia.ac.jp.
  • Sato M; Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
  • Hara S; Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
  • Yoshimoto Y; Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
  • Kondo R; Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioicho, Chiyoda-ku, Tokyo 102-8554, Japan.
  • Zimmermann S; Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland.
  • Kaiser M; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland.
  • Brun R; Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland.
  • Hamburger M; Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.
  • Adams M; Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences, University of Basel, Klingelbergstrasse 50, CH-4056 Basel, Switzerland.
Bioorg Med Chem Lett ; 24(3): 794-8, 2014 Feb 01.
Article em En | MEDLINE | ID: mdl-24433861
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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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sesquiterpenos / Tripanossomicidas / Trypanosoma brucei brucei / Lactonas Idioma: En Ano de publicação: 2014 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sesquiterpenos / Tripanossomicidas / Trypanosoma brucei brucei / Lactonas Idioma: En Ano de publicação: 2014 Tipo de documento: Article