New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms

New oxirane derivatives were synthesized using six naphthoquinones as the starting material. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxicity in the VERO cell line compared to naphthoquinones. In particular, oxirane de...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2012-08, Vol.20 (16), p.4995-5000
Hauptverfasser: Carneiro, Paula F., do Nascimento, Samara B., Pinto, Antonio V., Pinto, Maria do Carmo F.R., Lechuga, Guilherme C., Santos, Dilvani O., dos Santos Júnior, Helvécio M., Resende, Jackson A.L.C., Bourguignon, Saulo C., Ferreira, Vitor F.
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Sprache:eng
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Zusammenfassung:New oxirane derivatives were synthesized using six naphthoquinones as the starting material. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxicity in the VERO cell line compared to naphthoquinones. In particular, oxirane derivative 14 showed low cytotoxicity in a mammalian cell line and exhibited better activity against epimastigote forms of T.cruzi than the current drug used to treat Chagas disease, benznidazole New oxirane derivatives were synthesized using six naphthoquinones as the starting materials. Our biological results showed that these oxiranes acted as trypanocidal agents against Trypanosoma cruzi with minimal cytotoxicity in the VERO cell line compared to naphthoquinones. In particular, oxirane derivative 14 showed low cytotoxicity in a mammalian cell line and exhibited better activity against epimastigote forms of T.cruzi than the current drug used to treat Chagas disease, benznidazole.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2012.06.027