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Quinoxaline derivatives as antiparasitic drugs: proof of concept

Grant number: 13/50680-8
Support type:Research Grants - Research Partnership for Technological Innovation - PITE
Duration: November 01, 2014 - February 28, 2017
Field of knowledge:Physical Sciences and Mathematics - Chemistry
Cooperation agreement: GlaxoSmithKline
Principal Investigator:Arlene Gonçalves Corrêa
Grantee:Arlene Gonçalves Corrêa
Home Institution: Centro de Ciências Exatas e de Tecnologia (CCET). Universidade Federal de São Carlos (UFSCAR). São Carlos , SP, Brazil
Company: Glaxosmithkline Brasil Ltda
City: São Carlos
Associated scholarship(s):16/13894-8 - Quinoxaline derivatives as antiparasitic drugs: proof of concept, BP.PD
14/22548-0 - Quinoxaline derivatives as antiparasitic drugs: proof of concept, BP.PD

Abstract

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 Trypanossoma 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)

Scientific publications (4)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
COGO, JULIANA; CANTIZANI, JUAN; COTILLO, IGNACIO; SANGI, DIEGO PEREIRA; CORREA, ARLENE GONCALVES; UEDA-NAKAMURA, TANIA; DIAS FILHO, BENEDITO PRADO; JULIO MARTIN, JOSE; NAKAMURA, CELSO VATARU. Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents. Bioorganic & Medicinal Chemistry, v. 26, n. 14, p. 4065-4072, AUG 7 2018. Web of Science Citations: 0.
RODRIGUES, MARILI V. N.; BARBOSA, ALEXANDRE F.; DA SILVA, JULIA F.; DOS SANTOS, DEBORAH A.; VANZOLINI, KENIA L.; DE MORAES, MARCELA C.; CORREA, ARLENE G.; CASS, QUEZIA B. 9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors. Bioorganic & Medicinal Chemistry, v. 24, n. 2, p. 226-231, JAN 15 2016. Web of Science Citations: 11.
CORREA, ARLENE G.; PAIXAO, MARCIO W.; SCHWAB, RICARDO S. Application of Bio-Based Solvents in Catalysis. CURRENT ORGANIC SYNTHESIS, v. 12, n. 6, p. 675-695, 2015. Web of Science Citations: 23.
SANGI, DIEGO P.; COMINETTI, MARCIA R.; BECCENERI, AMANDA B.; RESENDE, FLAVIA A.; VARANDA, ELIANA A.; MONTANARI, CARLOS A.; PAIXAO, MARCIO W.; CORREA, ARLENE G. Molecular Design, Synthesis and Evaluation of 2,3-Diarylquinoxalines as Estrogen Receptor Ligands. Medicinal Chemistry, v. 11, n. 8, p. 736-746, 2015. Web of Science Citations: 0.

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