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

被引：29

作者：

Carneiro, Paula F. ^{[3
]}

do Nascimento, Samara B. ^{[1
,2
]}

Pinto, Antonio V. ^{[3
]}

Pinto, Maria do Carmo F. R. ^{[3
]}

Lechuga, Guilherme C. ^{[1
,2
]}

Santos, Dilvani O. ^{[1
,2
]}

dos Santos Junior, Helvecio M. ^{[5
]}

Resende, Jackson A. L. C. ^{[4
]}

Bourguignon, Saulo C. ^{[1
,2
]}

Ferreira, Vitor F. ^{[6
]}

机构：

[1] Univ Fed Fluminense, Lab Interacao Celular, Inst Biol, BR-24020150 Niteroi, RJ, Brazil

[2] Univ Fed Fluminense, Programa Posgrad Biol Interacoes, Inst Biol, BR-24020150 Niteroi, RJ, Brazil

[3] Univ Fed Rio de Janeiro, Nucleo Pesquisas Prod Nat, BR-21944970 Cidade Univ, RJ, Brazil

[4] Univ Fed Fluminense, Inst Quim, Dept Quim Inorgan, BR-24020150 Niteroi, RJ, Brazil

[5] Univ Fed Rio de Janeiro, Inst Quim, BR-21944970 Cidade Univ, RJ, Brazil

[6] Univ Fed Fluminense, Inst Quim, Dept Quim Organ, BR-24020150 Niteroi, RJ, Brazil

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 16期

关键词：

Naphthoquinone; Oxiranes; Trypanosoma cruzi; TRYPANOSOMA-CRUZI; TRYPANOCIDAL ACTIVITY; METAL-COMPLEXES; LAPACHONE; AGENTS; NAPHTHOQUINONES; GROWTH;

D O I：

10.1016/j.bmc.2012.06.027

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：4995 / 5000

页数：6

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