Avaliação citotóxica e leishmanicida in vitro de derivados sintéticos

• Autor(a) principal: Vieira, Ana Carolina Santana
• Data de Publicação: 2017
• Tipo de documento: Tese
• Idioma: por
• Título da fonte: Repositório Institucional da Universidade Federal de Alagoas (UFAL)
• Texto Completo: http://www.repositorio.ufal.br/handle/riufal/5831
• topic: Leishmaniose; Leishmania; Leishmania Chagasi; Leishmaniasis; CNPQ::CIENCIAS DA SAUDE::MEDICINA

Neglected diseases affect more than one billion people worldwide. Among them, leishmaniasis, which present in the visceral or integumentary forms. Caused by a protozoan of the genus Leishmania, they are endemic in 98 countries and do not yet have adequate treatment, representing a public health problem. The drugs of choice currently have adverse effects, besides the high cost, being important the research of new prototypes of drugs. The objective of this study was to evaluate the leishmanicidal activity of synthetic derivatives on Leishmania chagasi. Acyl oxymethyl derivatives synthesized from oxime ethers, vaniline derivatives and Morita-Baylis-Hillman adducts were evaluated. Leishmanicidal activity was verified by macrophages infection by promastigotes and then treated with different concentrations (0.1-100μM) of the derivatives. The results showed that all acyl oxymethyl derivatives showed leishmanicidal activity in the concentration of 30μM. The acyl oxymic derivativesTB06 (IC 50 27.7 ± 1.4), TB 08 (IC 50 17.3 ± 2.0) and TB 10 (IC 50 13.3 ± 6.7) showed 100% efficacy against amastigote forms. The results obtained in the evaluation of the Morita-Baylis-Hillman adducts show that the compounds 1G, 5G, 7G, 9G, 11G, 13G, 14G and 16G showed a significant reduction in the number of amastigotes in the 10μM concentration. Compounds 1G and 13G also showed leishmanicidal activity on promastigote forms of L. chagasi. Thus, it is concluded that acyl oxymethyl derivatives and Morita-Baylis-Hillman adducts are promising for the development of novel prototypes of leishmanicidal drugs.