期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 1, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126779
关键词
Neglected diseases; Chagas disease; Drug discovery; Azaindole
资金
- FAPESP [2015/19495-5, 2015/50655-9, 2013/07600-3]
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.
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