In vitro efficiency of new acridyl derivatives against Plasmodium falciparum

A series of new 9-substituted acridyl derivatives were synthesized and their in vitro antimalarial activity was evaluated against Plasmodium falciparum. Some compounds inhibit the growth of malarial parasite with IC 50 ⩽ 0.20 μM. A series of new 9-substituted acridyl derivatives were synthesized and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2007-05, Vol.15 (9), p.3278-3289
Hauptverfasser:	Guetzoyan, Lucie, Ramiandrasoa, Florence, Dorizon, Hélène, Desprez, Christine, Bridoux, Alexandre, Rogier, Christophe, Pradines, Bruno, Perrée-Fauvet, Martine
Format:	Artikel
Sprache:	eng
Schlagworte:	Acridines - chemical synthesis Acridines - chemistry Acridines - pharmacology Aminoacridine Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antimalarial Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Antiparasitic agents Biological and medical sciences Medical sciences Molecular Structure Parasitic Sensitivity Tests Peptidic synthesis Pharmacology. Drug treatments Plasmodium falciparum Plasmodium falciparum - drug effects Plasmodium falciparum - growth & development Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	A series of new 9-substituted acridyl derivatives were synthesized and their in vitro antimalarial activity was evaluated against Plasmodium falciparum. Some compounds inhibit the growth of malarial parasite with IC 50 ⩽ 0.20 μM. A series of new 9-substituted acridyl derivatives were synthesized and their in vitro antimalarial activity was evaluated against one chloroquine-sensitive strain (3D7) and three chloroquine-resistant strains [W2 (Indochina), Bre1 (Brazil) and FCR3 (Gambia)] of Plasmodium falciparum. Some compounds inhibit the growth of malarial parasite with IC 50 ⩽ 0.20 μM.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2007.02.022