Synthesis, characterization, antioxidant and antiparasitic activities new naphthyl-thiazole derivatives

Natali de França Nibbering Santos, Natanael da Silva Bezerra Junior, Jamerson Ferreira de Oliveira, Denise Maria Figueiredo Araújo Duarte, José Cleberson Dos Santos Soares, Diego Santa Clara Marques, Aline Caroline da Silva Santos, Fátima Nogueira, Valéria Rêgo Alves Pereira, Maria Carmo Alves de Lima, Iranildo José da Cruz Filho

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7 Citations (Scopus)
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Abstract

In this work, 13 thiosemicarbazones (1a - m) and 16 thiazoles (2a - p) were obtained, which were properly characterized by spectroscopic and spectrometric techniques. The pharmacokinetic properties obtained in silico revealed that the derivatives are in accordance with the parameters established by lipinski and veber, showing that such compounds have good bioavailability or permeability when administered orally. In assays of antioxidant activity, thiosemicarbazones showed moderate to high antioxidant potential when compared to thiazoles. In addition, they were able to interact with albumin and DNA. Screening assays to assess the toxicity of compounds to mammalian cells revealed that thiosemicarbazones were less toxic when compared to thiazoles. In relation to in vitro antiparasitic activity, thiosemicarbazones and thiazoles showed cytotoxic potential against the parasites Leishmania amazonensis and Trypanosoma cruzi. Among the compounds, 1b, 1j and 2l stood out, showing inhibition potential for the amastigote forms of the two parasites. As for the in vitro antimalarial activity, thiosemicarbazones did not inhibit Plasmodium falciparum growth. In contrast, thiazoles promoted growth inhibition. This study shows in a preliminary way that the synthesized compounds have antiparasitic potential in vitro.

Original languageEnglish
Article number108498
Pages (from-to)108498
Number of pages14
JournalExperimental Parasitology
Volume248
DOIs
Publication statusPublished - May 2023

Keywords

  • citotoxity in animal cells
  • Leishmania
  • Plasmodium falciparum
  • Thiazoles/pharmacology
  • Thiosemicarbazones/pharmacology
  • Trypanosoma cruzi

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