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New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity

Faist, Johanna and Hinteregger, Clemens and Seebacher, Werner and Saf, Robert and Mäser, Pascal and Kaiser, Marcel and Weis, Robert. (2017) New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity. Bioorganic & medicinal chemistry, 25 (3). pp. 941-948.

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Official URL: http://edoc.unibas.ch/54426/

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Abstract

Novel ω-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitrypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising. Some were equal or slightly more active than chloroquine against the sensitive strain. However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Mäser, Pascal and Kaiser, Marcel
Item Type:Article, refereed
Publisher:Pergamon
ISSN:0968-0896
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:31 Oct 2017 08:34
Deposited On:24 Apr 2017 13:57

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