In vitro and in vivo activities of multi-target phtalimido-thiazoles on Schistosomiasis mansoni.

Schistosomicidal activity of six phthalimido-thiazoles derivatives with substitutions at the position three of the thiazole ring were analyzed in an experimental model. The substituents biphenyl (2i) and 2- naphthyl (2j) at a concentration of 80 µg/mL caused 100% mortality of the parasite in culture after 24 h and 48 h respectively. An evaluation of ultrastructural parasites showed damage in the tegument, formation of bubbles and partial destruction of the tubercles. The in vivo anti-parasitic activity with the derivate 2i was performed by administering it orally and intraperitoneally in a 400 mg/kg/5days regimen. Decreases in the number of eggs in the gut (45.1%) and a reduction of the percentage of mature (23.7%) and increased unviable (53.8%) eggs were observed. Our results also showed a reduction in the number of recovered worms after treatment with 2i (oral administration: 81, 25%). The results demonstrated that the prototypes which were tested had a significant anti-schistosomal effect against S. mansoni, suggesting that these derivatives are promising candidates for further research into the chemotherapy of schistosomiasis. Copyright © 2020. Published by Elsevier B.V.

Citation

Carlos André Laranjeira Miranda Filho, Miria de Oliveira Barbosa, Arsênio Rodrigues Oliveira, Edna Farias Santiago, Veruska Cintia Alexandrino de Souza, Jéssica Paula Lucena, Camila Juliet Barbosa Fernandes, Ignes Regina Dos Santos, Renata Lins Carneiro Leão, Fabio André Brayner Dos Santos, Luiz Carlos Alves, Valéria Rego Alves Pereira, Roni Evêncio de Araújo, Ana Cristina Lima Leite, Sheilla Andrade de Oliveira. In vitro and in vivo activities of multi-target phtalimido-thiazoles on Schistosomiasis mansoni. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. 2020 Apr 15;146:105236

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PMID: 32058057

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