Trypanocidal activity of (−)-CUBEBIN (cas 18423-69-3) derivatives against free amastigote forms of Trypanosoma cruzi

Add time:09/08/2019    Source:sciencedirect.com

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.

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