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

[Display omitted] 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 co...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2020-01, Vol.30 (1), p.126779-126779, Article 126779
Main Authors: Koovits, Paul J., Dessoy, Marco A., Matheeussen, An, Maes, Louis, Caljon, Guy, Mowbray, Charles E., Kratz, Jadel M., Dias, Luiz C.
Format: Article
Language:English
Subjects:
Animals
Azaindole
Chagas disease
Chagas Disease - drug therapy
Drug discovery
Humans
Neglected diseases
Piperidines - pharmacology
Piperidines - therapeutic use
Structure-Activity Relationship
Trypanosoma cruzi - drug effects
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Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2019.126779