Literature DB >> 21940072

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

Esther del Olmo1, 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.   

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.
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID: 21940072     DOI: 10.1016/j.ejmech.2011.08.043

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  1 in total

1.  Enhanced antimalarial activity by a novel artemether-lumefantrine lipid emulsion for parenteral administration.

Authors:  Yufan Ma; Tingli Lu; Wen Zhao; Ying Wang; Ting Chen; Qibing Mei; Tao Chen
Journal:  Antimicrob Agents Chemother       Date:  2014-06-30       Impact factor: 5.191

  1 in total

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