New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity

AUTOR(ES)

SALVADOR, RAQUEL R.S., BELLO, MURILO L., BARRETO, IGOR R.L., VERA, MARIA A.F., MURI, ESTELA M.F., ALBUQUERQUE, SÉRGIO DE, DIAS, LUIZA R.S.

FONTE

An. Acad. Bras. Ciênc.

DATA DE PUBLICAÇÃO

01/12/2016

RESUMO

ABSTRACT 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.

Documentos Relacionados

• New 1-hydroxy-1,1-bisphosphonates derived from 1H-pyrazolo[3,4-b]pyridine: synthesis and characterization
• Synthesis of New Conjugates 1H-Pyrazolo[3,4-b]pyridine-phosphoramidate and Evaluation against Leishmania amazonensis
• On the one pot syntheses of chromeno[4,3-b]pyridine-3-carboxylate and chromeno[3,4-c]pyridine-3-carboxylate and dihydropyridines
• DFT study on low molecular weight α,α-ditert-butyl-4H-cyclopenta[2,1-b,3;4-b']dithiophene and α,α-ditert-butyl-4H-cyclopenta[2,1-b,3;4-b']dithiophene S-oxide bridged derivatives
• Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives