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ChemMedChem. 2019 Jan 3. doi: 10.1002/cmdc.201800691. [Epub ahead of print]

8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity.

Author information

1
Institut für Pharmazeutische und Medizinische Chemie, Heinrich-Heine-Universität Düsseldorf, Universitätsstrasse 1, 40225, Düsseldorf, Germany.
2
Institut für Tropenmedizin, Eberhard Karls Universität Tübingen, Wilhelmstrasse 27, 72074, Tübingen, Germany.
3
Eskitis Institute for Drug Discovery, Griffith University, Brisbane Innovation Park Campus, Nathan, QLD, 4111, Australia.
4
Department of Pediatrics, University of California San Diego, 9500 Gilman Drive, La Jolla, CA, 92037, USA.
5
Department of Life Sciences, Imperial College London, London, SW7 2AZ, UK.
6
Genomics Institute of the Novartis Research Foundation Department, Novartis, 10675 John Jay Hopkins Drive, San Diego, CA, 92121, USA.

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.

KEYWORDS:

8-aminoquinolines; antimalarials; dual-stage antiplasmodial activity; malaria

PMID:
30605243
DOI:
10.1002/cmdc.201800691

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