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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi

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Koovits, Paul J. [1] ; Dessoy, Marco A. [1] ; Matheeussen, An [2] ; Maes, Louis [2] ; Caljon, Guy [2] ; Mowbray, Charles E. [3] ; Kratz, Jadel M. [3] ; Dias, Luiz C. [1]
Total Authors: 8
[1] Univ Estadual Campinas, UNICAMP, Inst Chem, Rua Josue Castro S-N, Cidade Univ, BR-13083861 Campinas, SP - Brazil
[2] LMPH, Univ Pl 1, B-2610 Antwerp - Belgium
[3] DNDi, 15 Chemin Louis Dunant, CH-1202 Geneva - Switzerland
Total Affiliations: 3
Document type: Journal article
Source: Bioorganic & Medicinal Chemistry Letters; v. 30, n. 1 JAN 1 2020.
Web of Science Citations: 0

The structure-activity relationship of a 4-Azaindole-2-piperidine compound selected from GlaxoSmithKline's recently disclosed open-resource ``Chagas box{''} and possessing moderate activity against Trypanosoma cruzi, the parasite responsible for Chagas disease, is presented. Despite considerable medicinal chemistry efforts, a suitably potent and metabolically stable compound could not be identified to advance the series into in vivo studies. This research should be of interest to those in the area of neglected diseases and in particular anti-kinetoplastid drug discovery. (AU)

FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support type: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 15/50655-9 - FAPESP/MMV/DNDi/UNICAMP/USP Consortium to discover new drugs for the treatment of tropical parasitic diseases
Grantee:Luiz Carlos Dias
Support type: Research Grants - Research Partnership for Technological Innovation - PITE
FAPESP's process: 15/19495-5 - Compounds synthesis for the treatment of Chagas Disease at RIDCs/FAPESP/DNDi
Grantee:Paul John Koovits
Support type: Scholarships in Brazil - Post-Doctorate