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

Molecules

Shirani K. Haraguchi¹  Adriano A. Silva¹  Gentil J. Vidotti¹  Phercyles V. Dos Santos¹  Francielle P. Garcia¹  Raissa B. Pedroso¹  Celso V. Nakamura¹  Cecília M. A. De Oliveira¹ 

[1] ¹Departamento de Química, Universidade Estadual de Maringá, Av. Colombo, 5790, 87020-900, Maringá, PR, Brazil

关键词: kaurenoic acid;    thiosemicarbazone;    Trypanosoma cruzi;    Chagas desease;   

DOI  :  10.3390/molecules16021166

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.