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

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

Bioorganic & medicinal chemistry (2012-07-17)
Paula F Carneiro, Samara B do Nascimento, Antonio V Pinto, Maria do Carmo F R Pinto, Guilherme C Lechuga, Dilvani O Santos, Helvécio M dos Santos Júnior, Jackson A L C Resende, Saulo C Bourguignon, Vitor F Ferreira
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
1,4-Naphthoquinone, purum, ≥96.5% (HPLC)
Sigma-Aldrich
1,4-Naphthoquinone, 97%