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Title
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Novel quinoline derivatives with broad-spectrum antiprotozoal activities
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Author
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Abstract
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| 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 mu M, respectively, and with a high selectivity relative to human lung fibroblasts and mouse primary macrophages (similar to 100-fold). Compounds 2d and 4i also showed considerable activity against T. b. brucei with EC50 values of 1.4 and 0.4 mu M, respectively. Several quinoline derivatives incorporating arylnitro and aminochalcone moieties were synthesized and evaluated in vitro against a broad panel of trypanosomatid protozoan parasites. Compounds 2c, 2d, and 4i displayed submicromolar activity against Trypanosoma brucei rhodesiense, with high selectivity relative to human lung fibroblasts and mouse primary macrophages. image |
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Language
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English
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Source (journal)
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Archiv der Pharmazie. - Weinheim
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Publication
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Weinheim
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Wiley-v c h verlag gmbh
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2024
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ISSN
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0365-6233
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DOI
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10.1002/ARDP.202300319
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Volume/pages
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357
:6
(2024)
, p. 1-11
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Article Reference
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2300319
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ISI
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001169705500001
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Pubmed ID
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38396284
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Full text (Publisher's DOI)
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Full text (open access)
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