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Synthesis, leishmanicidal activity and theoretical evaluations of a series of substituted bis-2-hydroxy-1,4-naphthoquinones.

ABSTRACT: 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.

SUBMITTER: de Araujo MV 

PROVIDER: S-EPMC6271274 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature

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Synthesis, leishmanicidal activity and theoretical evaluations of a series of substituted bis-2-hydroxy-1,4-naphthoquinones.

de Araújo Morgana V MV   de Souza Patricia S O PS   de Queiroz Aline C AC   da Matta Carolina B B CB   Leite Anderson Brandão AB   da Silva Amanda Evelyn AE   de França José A A JA   Silva Tania M S TM   Camara Celso A CA   Alexandre-Moreira Magna S MS  

Molecules (Basel, Switzerland) 20140922 9

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 am  ...[more]

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