Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone
AbstractChagas disease is an endemic parasitic infection that occurs in 21 Latin American countries. New therapies for this disease are urgently needed, as the only two drugs available (nifurtimox and benznidazol) have high toxicity and variable efficacy in the disease’s chronic phase. Recently, a new chemical entity (NCE) named Pyranaphthoquinone (IVS320) was synthesized from lawsone. We report herein, a detailed study of the physicochemical properties and in vitro trypanocidal activity of IVS320. A series of assays were performed for characterization, where thermal, diffractometric, and morphological analysis were performed. In addition, the solubility, permeability, and hygroscopicity of IVS320 were determined. The results show that its poor solubility and low permeability may be due to its high degree of crystallinity (99.19%), which might require the use of proper techniques to increase the IVS320’s aqueous solubility and permeability. The trypanocidal activity study demonstrated that IVS320 is more potent than the reference drug benznidazole, with IC50/24 h of 1.49 ± 0.1 μM, which indicates that IVS320 has potential as a new drug candidate for the treatment of Chagas disease. View Full-Text
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Dantas, E.D.; de Souza, F.J.J.; Nogueira, W.N.L.; Silva, C.C.; de Azevedo, P.H.A.; Soares Aragão, C.F.; Almeida, P.D.O.; Cardoso, M.F.C.; da Silva, F.C.; de Azevedo, E.P.; Guimarães Barbosa, E.; Lima, E.S.; Ferreira, V.F.; Lima, Á.A.N. Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone. Molecules 2017, 22, 1631.
Dantas ED, de Souza FJJ, Nogueira WNL, Silva CC, de Azevedo PHA, Soares Aragão CF, Almeida PDO, Cardoso MFC, da Silva FC, de Azevedo EP, Guimarães Barbosa E, Lima ES, Ferreira VF, Lima ÁAN. Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone. Molecules. 2017; 22(10):1631.Chicago/Turabian Style
Dantas, Elen D.; de Souza, Fabia J.J.; Nogueira, William N.L.; Silva, Cláudia C.; de Azevedo, Pedro H.A.; Soares Aragão, Cícero F.; Almeida, Patricia D.O.; Cardoso, Mariana F.C.; da Silva, Fernando C.; de Azevedo, Eduardo P.; Guimarães Barbosa, Euzébio; Lima, Emerson S.; Ferreira, Vitor F.; Lima, Ádley A.N. 2017. "Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone." Molecules 22, no. 10: 1631.
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