Manganese(II) complexes with N4-methyl-4-nitrobenzaldehyde, N4-methyl-4-nitroacetofenone, and N4-methyl-4-nitrobenzophenone thiosemicarbazone: Investigation of in vitro activity against Trypanosoma cruzi
摘要:
Thiosemicarbazones are known to be active against different pathogenic microorganisms including Trypanosoma cruzi, the etiological agent of Chagas disease. In the search for new therapeutic drugs against this illness, the complexes [Mn(H4NO(2)Fo4M)(2)Cl-2] (1), [Mn(H(4)NO(2)Ac4M)(2)Cl-2] (2) and [Mn(H4NO(2) Bz4M)(2)Cl-2] (3) of N-4-methyl-4-nitrobenzaldehyde thiosemicarbazone (H4NO(2)Fo4M), N-4-methyl-4-nitroacetophenone thiosemicarbazone (H4NO(2)Ac4M) and N-4-methyl-4-nitrobenzophenone thiosemicarbazone (H4NO(2)Bz4M) were obtained and screened in vitro against bloodstream and intracellular forms of T. cruzi. H4NO(2)Fo4M, H4NO(2)Ac4M and their Mn(II) complexes displayed poor effect on bloodstream trypomastigotes, with IC50 values ranging from 68 to >200 mu M. However, although H4NO(2)Bz4M was also not active, its corresponding Mn(II) complex presented high effect on this T. cruzi form, with an IC50 value of 19 mu M. The effect of complex (3), against trypomastigotes of T. cruzi supports further in vitro as well as in vivo studies. (C) 2010 Elsevier Ltd. All rights reserved.