Title of article :
Trypanocidal activity of (−)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi
Author/Authors :
Vanessa A. de Souza، نويسنده , , Rosangela da Silva، نويسنده , , Ana C. Pereira، نويسنده , , Vanessa de A. Royo، نويسنده , , Juliana Saraiva، نويسنده , , Marisa Montanheiro، نويسنده , , Gustavo H.B. de Souza، نويسنده , , Ademar A. da Silva Filho، نويسنده , , Marcella D. Grando، نويسنده , , Paulo M. Donate، نويسنده , , Jairo K. Bastos، نويسنده , , Sérgio Albuquerque، نويسنده , , Marcio L.A. e Silva، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2005
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 (IC50 = 0.7 μM), and that 4 and 5 displayed moderate activity against the parasite, giving IC50 values of 5.7 and 4.7 μM, respectively. In contrast, it was observed that compound 3 was inactive and that 7 displayed low activity with IC50 values of 1.5 × 104 and 95.3 μM, respectively.
Keywords :
Amastigote forms , Lignans dibenzylbutyrolactones , Cubebin derivatives , Trypanocidal activity
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
