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Molecules 2017, 22(10), 1631;

Characterization and Trypanocidal Activity of a Novel Pyranaphthoquinone

Pharmacy Department, Health Sciences Center, Universidade Federal do Rio Grande do Norte (UFRN), Natal RN 59012-570, Brazil
Crowfoot Group of X-ray Techniques, Universidade Estadual do Amazonas (UEA), Manaus AM 69065-020, Brazil
Biological Activities Laboratory, Universidade Federal do Amazonas (UFAM), Pharmaceutical Sciences, Manaus AM 69080-900, Brazil
Laboratory of Synthesis of Bioactive Molecules, Organic Chemistry Department, Universidade Federal Fluminense (UFF), Niterói RJ 24020-141, Brazil
Graduate Program in Biotechnology, Laureate International Universities—Universidade Potiguar (UnP), Natal RN 59056-000, Brazil
Author to whom correspondence should be addressed.
Received: 12 September 2017 / Revised: 25 September 2017 / Accepted: 28 September 2017 / Published: 30 September 2017
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Chagas 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
Keywords: physicochemical characterization; IVS320; quinone; T. cruzi; Chagas disease; pyranaphthoquinone physicochemical characterization; IVS320; quinone; T. cruzi; Chagas disease; pyranaphthoquinone

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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.

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