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

Esther Del Olmo, Bianca Barboza, Louise D. Chiaradia, Alicia Moreno, Juana Carrero-Lérida, Dolores González-Pacanowska, Victoria Muñoz, José L. López-Pérez, Alberto Giménez, Agustín Benito, Antonio R. Martínez, Luis M. Ruiz-Pérez, Arturo San Feliciano

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

Abstract

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 IC 50 values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models.

Original languageEnglish
Pages (from-to)5379-5386
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number11
DOIs
StatePublished - Nov 2011

Keywords

  • Imidazoisoindoles
  • In vitro assays
  • In vivo assays
  • Mouse model
  • Plasmodium berghei
  • Plasmodium falciparum
  • Structure-activity relationship
  • Synthesis

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