Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
نویسندگان
چکیده
The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC(50) less than 1 microM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 microM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
منابع مشابه
Synthesis and Structure-Activity Relationship of 3-furyl and 3- thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives against Plasmodium falciparum
The aim of this study was to identify new active compounds against Plasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2carbonitrile 1,4-di-N-oxide derivatives. Antimalarial activity was evaluated in vitro against Plasmodium falciparum (3D7 and K1 strains) by the incorporation of [H]hypoxanthine. Cytotoxicity was tested in KB cells by Alamar Blue assay. Twelv...
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عنوان ژورنال:
- Molecules
دوره 13 1 شماره
صفحات -
تاریخ انتشار 2008