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

Structure-activity relationship

qui, 13 fev 2020

Publicado por


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 


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.

1   Institute of Chemistry, University of Campinas (UNICAMP), Rua Josué de Castro, S/N, Cidade Universitária, Campinas, SP 13083-861, Brazil

2   Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Universiteitsplein 1, 2610 Antwerpen, Belgium

3   Drugs for Neglected Diseases Initiative (DNDi), 15 Chemin Louis-Dunant, 1202 Geneva, Switzerland


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