Hochegger, Patrick and Faist, Johanna and Seebacher, Werner and Saf, Robert and Mäser, Pascal and Kaiser, Marcel and Weis, Robert. (2019) Synthesis and structure-activity relationships for new 6-fluoroquinoline derivatives with antiplasmodial activity. Bioorganic & medicinal chemistry, 27 (10). pp. 2052-2065.
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Official URL: https://edoc.unibas.ch/70288/
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Abstract
The substitution of 6-fluoroquinolines was modified in ring positions 2 and 4. The new compounds were tested in vitro for their activities against a sensitive and a multidrug resistant strain of Plasmodium falciparum. Some physicochemical parametres were calculated (log P, log D, ligand efficiency) or determined experimentally (permeability). The most promising compounds were tested for their in vivo activity against Plasmodium berghei in a mouse model. The 6-fluoro-2-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}-N-[2-(pyrrolidin-1-yl)ethyl]quinoline-4-carboxamide possessed proper physicochemical properties and showed high antiplasmodial activity in vitro (IC; 50; ≤ 0.0029 µM) and in vivo (99.6% activity).
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 (MPI) > Parasite Chemotherapy (Mäser) |
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UniBasel Contributors: | Mäser, Pascal and Kaiser, Marcel |
Item Type: | Article, refereed |
Article Subtype: | Research Article |
Publisher: | Pergamon |
ISSN: | 0968-0896 |
Note: | Publication type according to Uni Basel Research Database: Journal article |
Identification Number: |
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Last Modified: | 25 Apr 2019 08:30 |
Deposited On: | 25 Apr 2019 08:30 |
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