Synthesis, activity and molecular modeling studies of 1,2,3-triazole derivatives from natural phenylpropanoids as new trypanocidal agents.

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ID: 58114
2019
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Abstract
The search for compounds with new structural scaffolds is an important tool to the discovery of new drugs against Chagas disease. We report herein the synthesis of 1,2,3-triazoles obtained from eugenol and di-hydroeugenol and their in vitro and in vivo trypanocidal activity. These derivatives were obtained by a three-step objective route and were suitably characterized by H and C Nuclear Magnetic Resonance (NMR) spectroscopy and High Resolution Mass Spectrometry (HRMS). Two compounds (9 and 10) showed activity against epimastigote forms of Trypanosoma cruzi (Y strain) in the range 42.8-88.4 μM and were weakly toxic to cardiomyoblast cells (H9c2 cells). The triazole 10 was the most active derivative and could reduce more than 50% of parasitaemia after a 100 mg/kg oral treatment of mice infected with T. cruzi. Molecular docking studies suggested this compound could act as a trypanocidal agent by inhibiting cruzain, an essential enzyme for T. cruzi metabolism, usually inhibited by triazole compounds.
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de-souza2019synthesischemical Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors de Souza, Thiago Belarmino;Caldas, Ivo Santana;Paula, Favero Reisdorfer;Rodrigues, Camila Coelho;Carvalho, Diogo Teixeira;Dias, Danielle Ferreira;
Journal Chemical biology & drug design
Year 2019
DOI
10.1111/cbdd.13628
URL
Keywords
1,2,3-triazoles eugenol cruzain inhibitors di-hydroeugenol trypanocidal activity

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