Synthesis, Leishmanicidal Activity and Theoretical Evaluations of a Series of Substituted bis-2-Hydroxy-1,4-Naphthoquinones

被引：38

作者：

de Araujo, Morgana V. ^{[1
]}

de Souza, Patricia S. O. ^{[2
]}

de Queiroz, Aline C. ^{[1
]}

da Matta, Carolina B. B. ^{[1
]}

Leite, Anderson Brandao ^{[1
]}

da Silva, Amanda Evelyn ^{[1
]}

de Franca, Jose A. A. ^{[2
]}

Silva, Tania M. S. ^{[2
]}

Camara, Celso A. ^{[2
]}

Alexandre-Moreira, Magna S. ^{[1
]}

机构：

[1] Univ Fed Alagoas, Inst Biol Sci & Hlth, Lab Pharmacol & Immun, BR-57020720 Maceio, AL, Brazil

[2] Univ Fed Rural Pernambuco, Dept Mol Sci, Lab Bioact Cpds Synth, BR-52171900 Recife, PE, Brazil

来源：

MOLECULES | 2014年 / 19卷 / 09期

关键词：

naphthoquinones; knoevenagel; bis-2-hydroxy-1,4-naphthoquinones; antileishmanial activity; Leishmania braziliensis; Leishmania amazonensis; BETA-LAPACHONE; ANTILEISHMANIAL ACTIVITY; EFFICIENT SYNTHESIS; NAPHTHOQUINONES; DERIVATIVES; INHIBITION; CHEMISTRY;

D O I：

10.3390/molecules190915180

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：

A series of eight substituted bis-2-hydroxy-1,4-naphthoquinone derivatives was synthesized through lawsone condensation with various aromatic and aliphatic aldehydes under mild acidic conditions. The title compounds were evaluated for antileishmanial activity in vitro against Leishmania amazonensis and Leishmania braziliensis promastigotes; six compounds showed good activity without significant toxic effects. The compound with the highest activity was used for an in vivo assay with Leishmania amazonensis.

引用

页码：15180 / 15195

页数：16

共 37 条

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