Produção Nacional
Revisado por pares
In vivo antimalarial activity of novel 2-hydroxy-3-anilino-1,4-naphthoquinones obtained by epoxide ring-opening reaction
2013; Elsevier BV; Volume: 23; Issue: 16 Linguagem: Inglês
10.1016/j.bmcl.2013.06.033
ISSN1464-3405
AutoresLucas Cunha Dias de Rezende, Fernando Fumagalli, Marraiana Schiavon Bortolin, Marianne Garcia de Oliveira, Murilo Helder de Paula, Valter Ferreira de Andrade‐Neto, Flávio da Silva Emery,
Tópico(s)Malaria Research and Control
Resumo1,4-Naphthoquinone derivatives are known to have relevant activities against several parasites. Among the treatment options for malaria, atovaquone, a 1,4-naphthoquinone derivative, is widely applied in the treatment and prophylaxis of such disease. Based on the structure simplification of atovaquone, we designed and synthesized four novel naphthoquinoidal derivatives. The compounds were obtained by the underexplored epoxide-opening reaction of 1,4-naphthoquinone using aniline derivatives as nucleophiles. The antiplasmodial activity of the synthesized compounds was performed in vivo using Peter's 4days suppression test. Significant parasitemia reduction and increased survival were observed for some of the compounds.
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