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Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.

Abstract
Five (-)-cubebin derivative compounds, (-)-O-acetyl cubebin (3), (-)-O-benzyl cubebin (4), (-)-O-(N,N-dimethylaminoethyl)-cubebin (5), (-)-hinokinin (6) and (-)-6,6'-dinitrohinokinin (7), previously synthesised by our research group, were evaluated on in vitro assay against free amastigote forms of Trypanosoma cruzi, the asogic agent of Chagas' disease. It was observed that 6 was the most active compound (IC(50)=0.7 microM), and that 4 and 5 displayed moderate activity against the parasite, giving IC(50) values of 5.7 and 4.7 microM, respectively. In contrast, it was observed that compound 3 was inactive and that 7 displayed low activity with IC(50) values of congruent with 1.5 x 10(4) and 95.3 microM, respectively.
AuthorsVanessa A de Souza, Rosangela da Silva, Ana C Pereira, Vanessa de A Royo, Juliana Saraiva, Marisa Montanheiro, Gustavo H B de Souza, Ademar A da Silva Filho, Marcella D Grando, Paulo M Donate, Jairo K Bastos, Sérgio Albuquerque, Márcio L A e Silva
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 15 Issue 2 Pg. 303-7 (Jan 17 2005) ISSN: 0960-894X [Print] England
PMID15603944 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 6,6'-dinitrohinokinin
  • Benzodioxoles
  • Lignans
  • Membrane Glycoproteins
  • Protozoan Proteins
  • Trypanocidal Agents
  • amastin protein, Trypanosoma cruzi
  • cubebin
  • 4-Butyrolactone
Topics
  • 4-Butyrolactone (analogs & derivatives, chemistry, pharmacology, therapeutic use)
  • Animals
  • Benzodioxoles (chemistry, pharmacology, therapeutic use)
  • Chagas Disease (drug therapy)
  • Inhibitory Concentration 50
  • Lignans (chemistry, pharmacology, therapeutic use)
  • Membrane Glycoproteins (chemistry)
  • Parasitic Sensitivity Tests
  • Protozoan Proteins (chemistry)
  • Structure-Activity Relationship
  • Trypanocidal Agents (chemistry, pharmacology, therapeutic use)
  • Trypanosoma cruzi (drug effects)

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