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

Author(s)

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]

Affiliation

^[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

• Document type: Journal article
• Source: Bioorganic & Medicinal Chemistry Letters; v. 30, n. 1 JAN 1 2020.
• Web of Science Citations: 0

Abstract

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