1,4-萘醌新型环氧化衍生物及其对抗 T. cruzi 无鞭毛体形式的评价。
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
机构信息
Universidade Federal do Rio de Janeiro, Núcleo de Pesquisas de Produtos Naturais, 21944-970 Cidade Universitária, RJ, Brazil.
出版信息
Bioorg Med Chem. 2012 Aug 15;20(16):4995-5000. doi: 10.1016/j.bmc.2012.06.027. Epub 2012 Jun 21.
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.
我们使用六种萘醌作为起始原料合成了新的环氧化物衍生物。我们的生物学结果表明，与萘醌相比，这些环氧化物对 Trypanosoma cruzi 具有抗锥虫活性，同时细胞毒性最小。特别是，环氧化物衍生物 14 在哺乳动物细胞系中表现出低细胞毒性，并且对 T.cruzi 的前鞭毛体形式的活性优于用于治疗恰加斯病的现有药物苯并咪唑。
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