8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity
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Author(s)
Leven, Michael
Held, Jana
Duffy, Sandra
Avelar, Leandro A Alves
Meister, Stephan
Delves, Michael
Plouffe, David
Kuna, Krystina
Tschan, Serena
Avery, Vicky M
Winzeler, Elizabeth A
Mordmueller, Benjamin
Kurz, Thomas
Held, Jana
Duffy, Sandra
Avelar, Leandro A Alves
Meister, Stephan
Delves, Michael
Plouffe, David
Kuna, Krystina
Tschan, Serena
Avery, Vicky M
Winzeler, Elizabeth A
Mordmueller, Benjamin
Kurz, Thomas
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2019
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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.
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CHEMMEDCHEM
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14
Issue
4
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Medicinal and biomolecular chemistry
Organic chemistry
Pharmacology and pharmaceutical sciences