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Compounds synthesis for the treatment of Chagas Disease at RIDCs/FAPESP/DNDi

Grant number: 15/19495-5
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): March 01, 2016
Effective date (End): March 31, 2019
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Organic Chemistry
Principal Investigator:Luiz Carlos Dias
Grantee:Paul John Koovits
Home Institution: Instituto de Química (IQ). Universidade Estadual de Campinas (UNICAMP). Campinas , SP, Brazil
Associated research grant:13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery, AP.CEPID


The approach of this proposal is to use drug discovery leads from DNDi as starting points to deliver clinical candidates meeting the target product profiles (TPPs) for Chagas disease and visceral leishmaniasis (VL). The goal of this project is to deliver an optimised lead compound ready for preclinical and subsequently clinical development for the treatment of Chagas disease and/or visceral leishmaniasis (VL) that addresses the significant deficiencies of current standard of care medications. We will use the target product profiles (TPPs) developed by DNDi and its partners to ensure the deliverable is a compound that meets the needs of patients. The targeted clinical candidate will combine anti-protozoal efficacy with an acceptable safety profile and pharmacokinetics/physicochemical properties commensurate with oral delivery for testing against Chagas disease and/or a wide spectrum of manifestations of leishmaniasis, including visceral leishmaniasis. (AU)

Scientific publications
(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)
KOOVITS, PAUL J.; DESSOY, MARCO A.; MATHEEUSSEN, AN; MAES, LOUIS; CALJON, GUY; FERREIRA, LEONARDO L. G.; CHELUCCI, RAFAEL C.; MICHELAN-DUARTE, SIMONE; ANDRICOPULO, ADRIANO D.; CAMPBELL, SIMON; KRATZ, JADEL M.; MOWBRAY, CHARLES E.; DIAS, LUIZ C. Hit-to-lead optimization of a benzene sulfonamide series for potential antileishmanial agents. RSC MEDICINAL CHEMISTRY, v. 11, n. 11, p. 1267-1274, NOV 1 2020. Web of Science Citations: 0.
KOOVITS, PAUL J.; DESSOY, MARCO A.; MATHEEUSSEN, AN; MAES, LOUIS; CALJON, GUY; MOWBRAY, CHARLES E.; KRATZ, JADEL M.; DIAS, LUIZ C. Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi. Bioorganic & Medicinal Chemistry Letters, v. 30, n. 1 JAN 1 2020. Web of Science Citations: 0.

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