Synthesis and activity of some quinolone derivatives against Plasmodium falciparum in vitro.
Quinolones 7a-i and 8a-i were synthesized and tested in vitro as antimalarial against Plasmodium falciparum in chloroquine resistant strain. The above compounds were inactive at concentrations of 1.0 x 10(-4) M except the quinolone 3-amino-9-(2,4-dichlorophenyl)-1H-pyrazolo[3,4-b]-4-quinolone 7h which showed IC50 of 5.06 microM given the most interesting results.
Domínguez
J
J
Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Caracas, Venezuela.
Basante
W
W
Charris
J
J
Riggione
F
F
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004351:Drug Resistance; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010963:Plasmodium falciparum / Q000187:drug effects*; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000962:Antimalarials; D015363:Quinolones