某些喹诺酮衍生物对恶性疟原虫的体外合成及活性

Synthesis and activity of some quinolone derivatives against Plasmodium falciparum in vitro.

作者信息

Domínguez J, Basante W, Charris J, Riggione F

机构信息

Laboratorio de Síntesis Orgánica, Facultad de Farmacia, Universidad Central de Venezuela, Caracas, Venezuela.

出版信息

Farmaco. 1996 Jun;51(6):407-12.

PMID:8766223

Abstract

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.

摘要

合成了喹诺酮类化合物7a-i和8a-i，并在体外对氯喹抗性恶性疟原虫菌株进行了抗疟测试。除喹诺酮3-氨基-9-(2,4-二氯苯基)-1H-吡唑并[3,4-b]-4-喹诺酮7h外，上述化合物在浓度为1.0×10(-4) M时均无活性，该化合物的IC50为5.06 microM，给出了最有趣的结果。