Preparação e caracterização de derivados da 8-hidroxiquinolina e avaliação de suas atividades leishmanicidas utilizando a espécie Leishmania (Leishmania) amazonensis

• Ano de defesa: 2016
• Autor(a) principal: Silva, Etyene Janyne Gonzalez da [UNIFESP]
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Federal de São Paulo
• Palavras-chave em Português: Hydroxyquinoline; Functional group transformations; Quinoline derivatives; Leishmania (Leishmania) amazonensis; Leishmanicidal activity; Hidroxiquinolina; Transformações de grupos funcionais; Derivados quinolínicos; Atividade leishmanicida
• Link de acesso: https://sucupira.capes.gov.br/sucupira/public/consultas/coleta/trabalhoConclusao/viewTrabalhoConclusao.jsf?popup=true&id_trabalho=3795076; http://repositorio.unifesp.br/handle/11600/47018

Quinoline core is present in several biologically active substances. According to the literature 8-hydroxyquinoline has presented significant leishmanicidal activity against promastigote and amastigote forms of three species of Leishmania, including Leishmania (L.) amazonensis. Drugs used in the treatment of leishmaniasis have presented limitations such as, low efficiency and high toxicity, making necessary the searching for novel bioactive compounds. In this context, twenty-two compounds were evaluated against promastigote form of Leishmania (Leishmania) amazonensis, including three commercially available 8-hydroxyquinoline compounds and nineteen derivatives obtained through iodination, alkylation, and acylation reactions. The results of effective concentration 50% (EC50) obtained for the substances were compared with the EC50 value obtained for the amphotericin B, used as standard and, currently, employed in the treatment of leishmaniasis. The EC50 value obtained for 8-hydroxyquinoline was compared with the value described in the literature. Additionally, all compounds evaluated in this study showed leishmanicidal action with EC50 values ? 9.53 µg/mL, being considered biologically actives against promastigote form of L. (L.) amazonensis.