Antitrypanasomal activity of novel benzaldehyde-thiosemicarbazone derivatives from kaurenoic acid
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Data
2011-01
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Resumo
A series of new thiosemicarbazones derived from natural diterpene kaurenoic
acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to
evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones
were more active than kaurenoic acid with IC50 values between 2-24.0 mM. The o-nitrobenzaldehyde-
thiosemicarbazone derivative was the most active compound with IC50 of
2.0 mM. The results show that the structural modifications accomplished enhanced the
antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide
and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehydethiosemicarbazone
derivatives displayed lower toxicity for LLMCK2 cells than kaurenoic
acid, exhibing an IC50 of 59.5 mM.
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Kaurenoic acid, Thiosemicarbazone, Trypanosoma cruzi, Chagas desease
Citação
HARAGUCHI, Shirani K. et al. Antitrypanasomal activity of novel benzaldehyde-thiosemicarbazone derivatives from kaurenoic acid. Molecules, Basel, v. 16, p. 1166-1180, Jan. 2011.