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. 2024 Jun;357(6):e2300319.
doi: 10.1002/ardp.202300319. Epub 2024 Feb 23.

Novel quinoline derivatives with broad-spectrum antiprotozoal activities

Carla B Hartman  1 , Phelelisiwe S Dube  1 , Lesetja J Legoabe  1 , Natascha Van Pelt  2 , An Matheeussen  2 , Guy Caljon  2 , Richard M Beteck  1
Affiliations

Novel quinoline derivatives with broad-spectrum antiprotozoal activities

Carla B Hartman et al. Arch Pharm (Weinheim). 2024 Jun.

Abstract

Several quinoline derivatives incorporating arylnitro and aminochalcone moieties were synthesized and evaluated in vitro against a broad panel of trypanosomatid protozoan parasites responsible for sleeping sickness (Trypanosoma brucei rhodesiense), nagana (Trypanosoma brucei brucei), Chagas disease (Trypanosoma cruzi), and leishmaniasis (Leishmania infantum). Several of the compounds demonstrated significant antiprotozoal activity. Specifically, compounds 2c, 2d, and 4i displayed submicromolar activity against T. b. rhodesiense with half-maximal effective concentration (EC50) values of 0.68, 0.8, and 0.19 µM, respectively, and with a high selectivity relative to human lung fibroblasts and mouse primary macrophages (∼100-fold). Compounds 2d and 4i also showed considerable activity against T. b. brucei with EC50 values of 1.4 and 0.4 µM, respectively.

Keywords: anti‐infectives; arylnitro; chalcones; protozoal; quinoline.

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