Synthesis and biological evaluation of new compounds derived from primaquine for the treatment of Chagas Disease

• Grant number: 13/13172-4
• Support Opportunities: Scholarships in Brazil - Master
• Start date: May 01, 2014
• End date: July 31, 2015
• Field of knowledge: Health Sciences - Pharmacy - Medicines Analysis and Control
• Principal Investigator: Chung Man Chin
• Grantee: Diego Eidy Chiba
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Chagas disease, also known as American Tripanosomiasis, is caused by the hemoflagellate parasite Tripanosoma cruzi, is typically endemic in Latin and Central America, however, due to immigration process, this disease is present in other countries as United States and some countries in Europe. There are about 10 million people infected worldwide and more than 25 million people at risk of infection. The approved drugs for the treatment are benznidazol and nifurtimox, both of them are effective only in the acute phase of the disease. In Brazil, only benznidazol is available for the treatment. Due to that, this project aims to obtain hybrids compounds (or mutual prodrugs) of furoxans (and benzofuroxans) derivatives with primaquine. Furoxans and benzofuroxans derivatives show the capacity of donating nitric oxide, anti-inflammatory property and have been demonstrated interesting antiparasitic activity. Primaquine is an antimalarial drug and had been demonstrated potential against T. cruzi when used in a mutual prodrug with nitrofural, obtained by our group. The main structure planning is the substitution of the nitrofural compound (toxic) by furoxans and benzofuroxan in the new derivatives. Therefore, it is expected a synergic action in the elimination of the parasite. Will be obtained four new compounds and will be evaluated their activity against amastigote forms of T. cruzi, as well their mutagenic effect. (AU)

Academic Publications

(References retrieved automatically from State of São Paulo Research Institutions)

CHIBA, Diego Eidy. Síntese e avaliação biológica de novos compostos das séries LAPDESF FUR-PQ E LAPDESF FUR-TS contra Trypanosoma cruzi. 2015. Master's Dissertation - Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara Araraquara.