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

An Acad Bras Cienc

Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.

Published: February 2018

AI Article Synopsis

  • The paper investigates the trypanocidal activity of new carbohydrazide derivatives derived from a specific pyrazolo compound, focusing on their effectiveness against different forms of Trypanosoma cruzi.
  • The study found that the four carbohydrazide derivatives exhibited varying levels of antiparasitic activity, suggesting that their chemical structures play a significant role in their effectiveness.
  • Key factors influencing this activity include differences in lipophilicity and molecular volume, alongside their stereoelectronic properties and overall physical-chemical characteristics.

Article 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.

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http://dx.doi.org/10.1590/0001-3765201620160087DOI Listing

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