1. 8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity.
- Author
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Leven M, Held J, Duffy S, Alves Avelar LA, Meister S, Delves M, Plouffe D, Kuna K, Tschan S, Avery VM, Winzeler EA, Mordmüller B, and Kurz T
- Subjects
- Aminoquinolines chemical synthesis, Aminoquinolines pharmacology, Antimalarials chemical synthesis, Antimalarials pharmacology, Cell Survival drug effects, Hep G2 Cells, Humans, Life Cycle Stages drug effects, Plasmodium falciparum drug effects, Structure-Activity Relationship, Aminoquinolines chemistry, Antimalarials chemistry, Plasmodium falciparum growth & development
- Abstract
A series of novel 8-aminoquinolines (8-AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8-AQs bearing 2-alkoxy and 5-phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity., (© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Published
- 2019
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