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

• Grant number: 15/19495-5
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• Start date: March 01, 2016
• End date: March 31, 2019
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Luiz Carlos Dias
• Grantee: Paul John Koovits
• Host 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

Abstract

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; 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. (13/07600-3, 15/50655-9, 15/19495-5)

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; et al. 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. (15/50655-9, 15/19495-5, 13/07600-3)