title: Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds.
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.
authors.affiliation: Departamento de Química Farmacéutica, Facultad de Farmacia, CIETUS, Universidad de Salamanca, Spain. olmo@usal.es
authors.forename: Esther
authors.initials: E
authors.lastname: del Olmo
authors.forename: Bianca
authors.initials: B
authors.lastname: Barboza
authors.forename: Louise D
authors.initials: LD
authors.lastname: Chiaradia
authors.forename: Alicia
authors.initials: A
authors.lastname: Moreno
authors.forename: Juana
authors.initials: J
authors.lastname: Carrero-Lérida
authors.forename: Dolores
authors.initials: D
authors.lastname: González-Pacanowska
authors.forename: Victoria
authors.initials: V
authors.lastname: Muñoz
authors.forename: José L
authors.initials: JL
authors.lastname: López-Pérez
authors.forename: Alberto
authors.initials: A
authors.lastname: Giménez
authors.forename: Agustín
authors.initials: A
authors.lastname: Benito
authors.forename: Antonio R
authors.initials: AR
authors.lastname: Martínez
authors.forename: Luis M
authors.initials: LM
authors.lastname: Ruiz-Pérez
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D001554:Benzene / Q000737:chemistry; D002460:Cell Line; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D020128:Inhibitory Concentration 50; D054833:Isoindoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D008297:Male; D051379:Mice; D018512:Parasitemia / Q000188:drug therapy; D010962:Plasmodium berghei / Q000187:drug effects / Q000472:pathogenicity; D010963:Plasmodium falciparum / Q000187:drug effects
chemical_list: D000962:Antimalarials; D007093:Imidazoles; D054833:Isoindoles; D001554:Benzene