Artículos de revistas
Synthesis, Antitubercular and Leishmanicidal Evaluation of Resveratrol Analogues
Fecha
2016-12-01Registro en:
Journal Of The Brazilian Chemical Society. Sao Paulo: Soc Brasileira Quimica, v. 27, n. 12, p. 2161-2169, 2016.
0103-5053
10.5935/0103-5053.20160107
S0103-50532016001202161
WOS:000391146000001
S0103-50532016001202161.pdf
Autor
Univ Fed Juiz de Fora
Universidade Estadual Paulista (Unesp)
Institución
Resumen
In this paper we continue our efforts in the search for new Schiff bases as resveratrol analogues as promising antitubercular and antileishmanial agents. Compounds were evaluated in vitro against Mycobacterium tuberculosis and Leishmania species. Compounds showed varying activity against promastigotes of all Leishmania species tested (concentration leading to reduction of 50% of parasite growth-IC50 values ranging from 1.60 to 15.53 mu g mL(-1)). Majority of compounds exhibited good results against Leishmania species with IC50 values below 10.00 mu g mL(-1), with no cytotoxicity against macrophages. One of the analogues showed the best activity against amastigotes of L. amazonensis (IC50 = 5.73 mu g mL(-1)). Furthermore, the compounds showed comparable or better effect than drugs commonly used in tuberculosis treatment such as Cycloserine (R). The analogue that was the most active for M. tuberculosis had minimal inhibitory concentration MIC90=0.78 mu gmL(-1). The in vitro cytotoxicity on Vero cells (CC50), as well as the selectivity index (SI = CC50/MIC) were also evaluated, and showed that the synthesized analogues are not cytotoxic.