Nitroquinolones and nitroquinolines: syntheses and antitrypanosomal activity.

Authors

Phelelisiwe S Dube, Karol R Francisco, Lesetja J Legoabe, Yujie Uli Sun, Yashpreet Kaur, Tina P Nguyen, Conor R Caffrey, Richard M Beteck

Published in

Molecular diversity. Nov 21, 2025. Epub Nov 21, 2025.

Abstract

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.

PMID:
41269570
Bibliographic data and abstract were imported from PubMed on 21 Nov 2025.

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