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

26 jun 2020

Paul J. Koovits, Marco A. Dessoy, An Matheeussen, Luis Maes, Guy Caljon, Charles E. Mowbray, Jadel M. Kratz, Luiz C. Dias

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.

https://doi.org/10.1016/j.bmcl.2019.126779