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Quinoxaline derivatives as antiparasitic drugs: proof of concept

Grant number: 14/22548-0
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): March 01, 2015
Effective date (End): April 30, 2016
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Cooperation agreement: GlaxoSmithKline
Principal researcher:Arlene Gonçalves Corrêa
Grantee:Gustavo Frensch
Home Institution: Centro de Ciências Exatas e de Tecnologia (CCET). Universidade Federal de São Carlos (UFSCAR). São Carlos , SP, Brazil
Company:Universidade Federal de São Carlos (UFSCAR). Centro de Ciências Exatas e de Tecnologia (CCET)
Associated research grant:13/50680-8 - Quinoxaline derivatives as antiparasitic drugs: proof of concept, AP.PITE


Quinoxalines are a class of heterocyclic compounds that have been intensively studied for their biological activities, showing promising activity against protozoa. In an ongoing study towards the discovery of new antiparasitic compounds, we have synthesized a library of quinoxaline derivatives, which has been evaluated in vitro against epimastigote, promastigote, and trypomastigote forms of Trypanosoma cruzi and intracellular amastigote and promastigote forms of Leishmania amazonensis. From this screening, we have selected the most active compounds for in vivo and mechanistic studies. The main objective of this project is to prove the biological activity of these compounds in the drug development for tropical diseases such as Chagas' disease and leishmaniasis. More specifically, our goal is the synthesis of quinoxaline derivatives aiming at improving yield, a scalable and safe process and decreasing of chemical residues. Looking into pharmaceutical application of these drug candidates, they will be evaluated in vitro and in vivo in order to determine their mechanism of action against T. cruzi and L. amazonensis. (AU)

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