Publication
Title
Novel quinoline derivatives with broad-spectrum antiprotozoal activities
Author
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 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
Language
English
Source (journal)
Archiv der Pharmazie. - Weinheim
Publication
Weinheim : Wiley-v c h verlag gmbh , 2024
ISSN
0365-6233
DOI
10.1002/ARDP.202300319
Volume/pages
(2024) , 11 p.
Article Reference
e2300319
ISI
001169705500001
Pubmed ID
38396284
Full text (Publisher's DOI)
Full text (open access)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identifier
Creation 29.03.2024
Last edited 04.04.2024
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