Novel quinoline derivatives with broad-spectrum antiprotozoal activities.
Arch Pharm (Weinheim)
; 357(6): e2300319, 2024 Jun.
Article
in En
| MEDLINE
| ID: mdl-38396284
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 (â¼100-fold). Compounds 2d and 4i also showed considerable activity against T. b. brucei with EC50 values of 1.4 and 0.4 µM, respectively.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Quinolines
/
Trypanosoma cruzi
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Trypanosoma brucei rhodesiense
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Leishmania infantum
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Parasitic Sensitivity Tests
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Antiprotozoal Agents
Limits:
Animals
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Humans
Language:
En
Journal:
Arch Pharm (Weinheim)
Year:
2024
Document type:
Article
Affiliation country:
South Africa
Country of publication:
Germany