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As a continuation of our research and with the aim of obtaining new antimalarial agents, new series of 3-phenylquinoxaline 1,4-di-N-oxide derivatives have been synthesized following the classical Beirut reaction. Antiplasmodial activity was evaluated in vitro against Plasmodium falciparum by the incorporation of [ 3 H]-hypoxanthine. Cytotoxicity was tested in KB cells by AlamarBlue assay. Twenty-one of the 60 compounds that were assayed against 3D7 (CQ-sensitive) showed enough activity to be also evaluated against K1 (CQ-resistant) strain. Ten of them were shown to be more active than chloroquine in the resistant strain. The most interesting compounds are 7-(methyl or methoxy)-3-(4′-fluoro or chloro)phenylquinoxaline-2-carbonitrile 1,4-di-N-oxides because of their low IC 50 and their high SI shown for the K1 strain, making them valid new leads. © 2007 Elsevier Masson SAS. All rights reserved.

Original publication

DOI

10.1016/j.ejmech.2007.11.024

Type

Journal article

Journal

European Journal of Medicinal Chemistry

Publication Date

01/09/2008

Volume

43

Pages

1903 - 1910