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

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

Bioorganic & medicinal chemistry letters 2020 Jan 01

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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. Copyright © 2019 The Authors. Published by Elsevier Ltd.. All rights reserved.

Citation

Paul J Koovits, Marco A Dessoy, An Matheeussen, Louis Maes, Guy Caljon, Charles E Mowbray, Jadel M Kratz, Luiz C Dias. Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi. Bioorganic & medicinal chemistry letters. 2020 Jan 01;30(1):126779