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Updated: Jan 6, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Nitroquinolones and nitroquinolines: syntheses and antitrypanosomal activity
Phelelisiwe S Dube1, Karol R Francisco2, Lesetja J Legoabe1
1Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, 2520, South Africa.
None:
Nitroaromatic small molecules are established anti-infectives, including against trypanosomal diseases. Inspired by our previously identified suicide inhibitors of Mycobacterium tuberculosis (Mtb) decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1), we report the synthesis and in vitro antitrypanosomal activity of six novel nitroquinoline derivatives (4a-4f), as well as the antitrypanosomal activity of 13 previously described nitroquinolone anti-Mtb compounds, 8a-8 m. Two compounds exhibited sub-micromolar activity (EC50 = 0.3-0.5 µM), while thirteen compounds exhibited low micromolar activity (EC50 = 1.1-8.0 µM) against Trypanosoma brucei. This study highlights nitroquinolones and nitroquinolines as a source of compounds that exhibit both antitrypanosomal and antitubercular activities.
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