Anais da Academia Brasileira de Ciências
versão impressa ISSN 0001-3765
versão On-line ISSN 1678-2690
SALVADOR, RAQUEL R.S. et al. New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity. An. Acad. Bras. Ciênc. [online]. 2016, vol.88, n.4, pp.2341-2348. Epub 01-Dez-2016. ISSN 0001-3765. http://dx.doi.org/10.1590/0001-3765201620160087.
This paper reports the in vitro trypanocidal activity evaluation of new carbohydrazide derivatives from 3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine, substituted at C-6 position by phenyl, methyl or trifluoromethyl group. These compounds were evaluated in order to identify the antiparasitic profile against trypomastigote and amastigote forms of Trypanosoma cruzi. The 4-carbohydrazide derivatives presented different profiles of activity. In the investigation of the chemical structure influence in the trypanocidal activity, the results indicated there are large lipophilicity and volume differences among these derivatives. The complementarities of their stereoelectronic and physical-chemical aspects seem to be relevant for the biological activity against T. cruzi.
Palavras-chave : 1H-pyrazolo[3,4-b]pyridine; carbohydrazide derivatives; biological activities; trypanocidal activity; molecular modeling.