Article
Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues
Registro en:
FERREIRA, Sabrina Baptista; et al. Synthesis and anti-Trypanosoma cruzi activity of b-lapachone analogues. European Journal of Medicinal Chemistry, v.46, p.3071-3077, 2011.
0223-5234
10.1016/j.ejmech.2011.03.012
1768-3254
Autor
Ferreira, Sabrina Baptista
Salomão, Kelly
Silva, Fernando de Carvalho da
Pinto, Antônio Ventura
Kaiser, Carlos Roland
Pinto, Angelo C.
Ferreira, Vitor Francisco
Castro, Solange L. de
Resumen
The available chemotherapy for Chagas disease, caused by Trypanosoma cruzi, is unsatisfactory; therefore, there is an intense effort to find new drugs for the treatment of this disease. In our laboratory, we have analyzed the effect on bloodstream trypomastigotes of 16 new naphthoquinone analogues of β-lapachone modified in the pyran ring, aiming to find a new prototype with high trypanocidal activity. The new compounds presented a broad spectrum of activity, and five of them presented IC(50)/24 h in the range of 22-63 μM, whereas β-lapachone had a higher value of 391.5 ± 16.5 μM. 2030-01-01