Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
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.
de Souza
Vanessa A
VA
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas da Universidade de Franca, Av. Dr. Armando Salles de Oliveira, 2001, CEP: 14404-600, Franca, SP, Brazil.
da Silva
Rosangela
R
Pereira
Ana C
AC
Royo
Vanessa de A
Vde A
Saraiva
Juliana
J
Montanheiro
Marisa
M
de Souza
Gustavo H B
GH
da Silva Filho
Ademar A
AA
Grando
Marcella D
MD
Donate
Paulo M
PM
Bastos
Jairo K
JK
Albuquerque
Sérgio
S
e Silva
Márcio L A
ML
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D052117:Benzodioxoles / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D014355:Chagas Disease / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D017705:Lignans / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D008562:Membrane Glycoproteins / Q000737:chemistry*; D021261:Parasitic Sensitivity Tests; D015800:Protozoan Proteins / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D014349:Trypanosoma cruzi / Q000187:drug effects*
C000605643:6,6'-dinitrohinokinin; D052117:Benzodioxoles; D017705:Lignans; D008562:Membrane Glycoproteins; D015800:Protozoan Proteins; D014344:Trypanocidal Agents; C088681:amastin protein, Trypanosoma cruzi; C433065:cubebin; D015107:4-Butyrolactone