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Synthesis and Antimalarial Properties of New Chloro-9H-xanthones with an Aminoalkyl Side Chain

✍ Scribed by César Portela; Carlos M. M. Afonso; Madalena M. M. Pinto; Dinora Lopes; Fátima Nogueira; Virgílio do Rosário

Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
133 KB
Volume
4
Category
Article
ISSN
1612-1872

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✦ Synopsis

Abstract

The synthesis and antimalarial properties of twelve new chlorinated 9__H__‐xanthones, carrying a [2‐(diethylamino)ethyl]amino group in position 1, are reported. All compounds were found to be active towards the chloroquine‐susceptible and chloroquine‐resistant strains 3D7 and Dd2, resp., of the protozoa parasite Plasmodium falciparum. Especially one compound, 6‐chloro‐1‐{[2‐(diethylamino)ethyl]amino}‐9__H__‐xanthen‐9‐one (1k), was found to exhibit significant in vitro activity (IC~50~=3.9 μM) towards the resistant Dd2 strain.

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