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Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds

AuthorsOlmo, Esther del; Barboza, B.; Chiaradia, L. D.; Moreno, A.; Carrero-Lérida, J.; González-Pacanowska, D.; Muñoz, V.; López-Pérez, J. L.; Giménez, Alberto P.; Benito, Agustín; Martínez, A. R.; Ruiz-Pérez, Luis Miguel; San Feliciano, A.
Issue Date2011
CitationEuropean Journal of Medicinal Chemistry 46: 5379- 5386 (2011)
AbstractThe 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. © 2011 Elsevier Masson SAS. All rights reserved.
Identifiersdoi: 10.1016/j.ejmech.2011.08.043
issn: 0223-5234
Appears in Collections:(IPBLN) Artículos
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