Document Report Card

Basic Information

ID: ALA1833920

Journal: Eur J Med Chem

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

Authors: del Olmo E, Barboza B, Chiaradia LD, Moreno A, Carrero-Lérida J, González-Pacanowska D, Muñoz V, López-Pérez JL, Giménez A, Benito A, Martínez AR, Ruiz-Pérez LM, San Feliciano A.

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.

CiteXplore: 21940072

DOI: 10.1016/j.ejmech.2011.08.043