Synthesis and protozoocidal activity of new 1,4-naphthoquinones

被引:0
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作者
Danoun, S
Baziard-Mouysset, G
Stigliani, JL
Ané-Margail, M
Payard, M
Léger, JM
Canron, X
Vial, H
Loiseau, PM
Bories, C
Récoché, C
机构
[1] Fac Pharm, Lab Chim Pharmaceut, F-31062 Toulouse, France
[2] UFR Pharm, Lab Chim Analyt & Cristallog, F-33076 Bordeaux, France
[3] Dept Biol Sante, F-34095 Montpellier, France
[4] Fac Pharm, Parasitol Lab, F-92290 Chatenay Malabry, France
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Four naphthoquinones were submitted to the action of diazomethane. The structure of the nine adducts, of which four were original, was determined. The protozoocidal activity of these compounds was evaluated in vitro against Plasmodium falciparum, Leishmania donovani, Trypanosoma brucei and Trichomonas vaginalis. The 2-methoxy-naphthoquinone <(3a)under bar> exhibited some activity and was more potent against these four protozoa than the reference drugs. The 2-methoxynaphthoquinone <(4a)under bar> showed more activity than chloroquine towards Plasmodium falciparum.
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页码:343 / 348
页数:6
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