期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 11, 页码 5379-5386出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.08.043
关键词
Synthesis; Imidazoisoindoles; In vitro assays; Plasmodium falciparum; Structure-activity relationship; In vivo assays; Mouse model; Plasmodium berghei
资金
- ALFA [ALR/B73011/94.04-6.0275.9]
- ALBAN [E07D401988BR]
- EC
- Plan Andaluz de Investigacion [BIO199]
- ISCIII-RICET [RD06/0021: 0000, 0018, 0022]
- [FIS-PI-060782]
- [FIS-PI-052026]
- [SAF2010-20059]
The synthesis of several series of imidazo[2,1-a]isoindol-5-ol derivatives and the results of their evaluation against Plasmodium falciparum are presented and discussed. The effects of electron-withdrawing or-donating substituents on different parts of the molecule, as well as those produced by the incorporation of an additional fused ring, were analyzed. Several compounds showed significant antimalarial activity in vitro with IC50 values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models. (C) 2011 Elsevier Masson SAS. All rights reserved.
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