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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 (EC 50 ) 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 EC 50 values of 1.4 and 0.4 µM, respectively.
Hartman et al. (Fri,) studied this question.