Síntese e avaliação biológica de novos compostos das séries LAPDESF FUR-PQ E LAPDESF FUR-TS contra Trypanosoma cruzi

• Ano de defesa: 2015
• Autor(a) principal: Chiba,Diego Eidy [UNESP]
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Estadual Paulista (Unesp)
• Palavras-chave em Português: Fármacos; Chagas, Doença de; Barbeiro (Inseto); Reduviidae; Triatoma; Cromatografia em camada fina; Trypanosoma cruzi
• Link de acesso: http://hdl.handle.net/11449/139367; http://www.athena.biblioteca.unesp.br/exlibris/bd/cathedra/31-05-2016/000864103.pdf

Chagas disease, also known as American trypanosomiasis, caused by the hemoflagellate parasite Trypanosoma cruzi, is typically endemic in countries of Central and Latin America. However, due to the migration process, this disease has already reached other countries like the United States and some European countries. It is estimated that there are approximately 7 - 8 million people infected worldwide and more than 25 million are at risk of infection. The drugs approved for the treatment are benznidazole and nifurtimox, both active only in the acute phase of the disease. In Brazil, only benznidazole is available. Due to the above, this project proposes to obtain two series of compounds. The Series 1 consists of seven new compounds derived from furoxanos and primaquine. The second series consists of six new bioisosters of nitrofurazone, replacing the nitrofuran group with furoxan. Furoxans derivatives have the ability to donate NO, anti-inflammatory properties and have shown interesting anti-parasitic activity. Primaquine is an antimalarial drug, which was previously demonstrated to have potential trypanocidal activity. Six furoxans intermediates and six finals derivatives were synthesized and characterized by infrared spectrometry (IR) and Nuclear Magnetic Resonance (NMR). Was evaluated the trypanocidal activity against epimastigote form of T. cruzi, the capability of NO donation and the mutagenicity in an in vivo assay. They presented good activity against epimastigote forms of parasite and show no mutagenicity in the in vivo assay.