Indolone-N-oxide derivatives: in vitro activity against fresh clinical isolates of Plasmodium falciparum, stage specificity and in vitro interactions with established antimalarial drugs | Zendy

Rachida Tahar | Zendy; Livia Vivas | Zendy; Léonardo K. Basco | Zendy; Elizabeth Thompson | Zendy; Hany Ibrahim | Zendy; Jérémie Boyer | Zendy; F. Nepveu | Zendy

Open Access

Indolone-N-oxide derivatives: in vitro activity against fresh clinical isolates of Plasmodium falciparum, stage specificity and in vitro interactions with established antimalarial drugs

Author(s) -

Rachida Tahar,

Livia Vivas,

Léonardo K. Basco,

Elizabeth Thompson,

Hany Ibrahim,

Jérémie Boyer,

F. Nepveu

Publication year - 2011

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkr320

Subject(s) - dihydroartemisinin , plasmodium falciparum , pharmacology , artemisinin , amodiaquine , chloroquine , mefloquine , in vitro , quinine , lumefantrine , biology , chemistry , stereochemistry , malaria , biochemistry , immunology

Indolone-N-oxides are characterized by the presence of a highly reactive pharmacophore, the nitrone moiety (C=N(+)-O(-)), which undergoes oxidation-reduction reactions. The aims of the present study were to: (i) evaluate the in vitro activity of the parent compound, designated as compound 1, against 34 fresh clinical isolates of Plasmodium falciparum; (ii) compare the activity of compound 1 with that of chloroquine and dihydroartemisinin to assess the potential for cross-resistance; (iii) investigate drug interactions of indolone-N-oxides with standard antimalarials; and (iv) determine the stage-dependent activity of indolone-N-oxides.

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