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Molecules ; 16(2): 1166-80, 2011 Jan 26.
Artigo em Inglês | MEDLINE | ID: mdl-21270733

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-nitro-benzaldehyde-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-chlorobenzaldehyde-thiosemicarbazone derivatives displayed lower toxicity for LLMCK2 cells than kaurenoic acid, exhibing an IC50 of 59.5 mM.


Assuntos
Benzaldeídos/química , Diterpenos/química , Tiossemicarbazonas/química , Tripanossomicidas/química , Animais , Benzaldeídos/farmacologia , Concentração Inibidora 50 , Estrutura Molecular , Tiossemicarbazonas/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos
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