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Design, synthesis and biological evaluation of drug candidates for the treatment of Chagas Disease and Leishmaniasis

Grant number: 13/01618-8
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): August 01, 2013
Effective date (End): February 23, 2014
Field of knowledge:Health Sciences - Pharmacy - Medicines Analysis and Control
Principal Investigator:Chung Man Chin
Grantee:Priscila Longhin Bosquesi
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Neglected diseases are those that affect thousands of people around the world, but lack of adequate or effective treatments. Between 1975 and 2004, a total of 1556 new drugs approved, only 21 (1.3%) of the drugs that entered the market were for neglected diseases. For more than a century of his description, Chagas disease remains a major public health problems. Resulting from infection flagellate protozoan Trypanosoma cruzi, is endemic in 21 countries of Latin America and it is estimated that 10 million people are infected and about 100 million are at risk of contamination. Two drugs are available for treating the disease, nifurtimox and benznidazole. Both active only in the acute phase of the disease. In Brazil is marketed only benznidazole. Leishmaniasis affects 12 million people worldwide and endanger approximately 350 million. The chemotherapy of leishmaniasis relies on the use of compounds pentavalent antimonials, which are toxic and present inefficiency due to infection of patients by resistant strains. For the above, design and synthesis of new drugs for the treatment of neglected diseases and neglected by government agencies and universities, especially Brazil, is of paramount importance. Once the compounds are derived furoxanos and benzofuroxans generating compounds reactive oxygen species and in recent years has shown potential antiparasitic activity this project proposes the design, synthesis and biological evaluation of 24 compounds, isosteres nitrofurazone and hydroxymethylnitrofurazone, for the treatment of Chagas disease and Leishmaniasis. (AU)