Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid †

Shirani K. Haraguchi, Adriano A. Silva, Gentil J. Vidotti, Phercyles V. Dos Santos, Francielle P. Garcia, Raissa B. Pedroso, Celso V. Nakamura, Cecília M. A. De Oliveira, Cleuza C. Da Silva
2011 Molecules  
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 IC 50 values between 2-24.0 µM. The o-nitrobenzaldehyde-thiosemicarbazone derivative was the most active compound with IC 50 of 2.0 µM. The results show that the structural modifications accomplished
more » ... 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 LLMCK 2 cells than kaurenoic acid, exhibing an IC 50 of 59.5 µM. OPEN ACCESS Molecules 2011, 16 1167
doi:10.3390/molecules16021166 pmid:21270733 fatcat:72ty7kmblff63c7xgjts5wq5gy