Application of multicomponent reactions to antimalarial drug discovery. Part 3: Discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro


Musonda, CC; Little, S; Yardley, V; Chibale, K; (2007) Application of multicomponent reactions to antimalarial drug discovery. Part 3: Discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro. Bioorganic & medicinal chemistry letters, 17 (17). pp. 4733-4736. ISSN 0960-894X DOI: https://doi.org/10.1016/j.bmcl.2007.06.070

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Abstract

The synthesis and antimalarial activity of a novel series of first generation 4-aminoquinoline-containing 2,4,5-trisubstituted aminoxazoles against two strains of the Plasmodium falciparum parasite in vitro is described. A number of compounds significantly more potent than the standard drug chloroquine were identified. (c) 2007 Elsevier Ltd. All rights reserved.

Item Type: Article
Keywords: Aminoquinolines, chemistry, Animals, Antimalarials, chemical synthesis, pharmacology, Chemistry, Pharmaceutical, methods, Drug Design, Drug Evaluation, Preclinical, Inhibitory Concentration 50, Oxazoles, chemistry, Parasitic Sensitivity Tests, Plasmodium, metabolism, Plasmodium falciparum, drug effects, Structure-Activity Relationship
Faculty and Department: Faculty of Infectious and Tropical Diseases > Dept of Immunology and Infection
Faculty of Infectious and Tropical Diseases > Dept of Clinical Research
PubMed ID: 17644333
Web of Science ID: 249151700002
URI: http://researchonline.lshtm.ac.uk/id/eprint/8434

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