title: The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds.
abstract: The in vitro antiplasmodial activity of some dihydrostilbenamides, phtalazinones, imidazo[2,1-a]isoindole and pyrimido[2,1-a]isoindole derivatives related to the natural dihydrostilbenoid isonotholaenic acid is reported. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum and potent representative compounds were also evaluated in the ferriprotoporphyrin IX biomineralization inhibition test (FBIT). Compounds having the imidazo[2,1-a]isoindole skeleton were the most active and one compound of this group resulted to be as potent as chloroquine, but acting through a mechanism different that of the inhibition of heme biomineralization.
authors.affiliation: Departamento de Química Farmacéutica, Facultad de Farmacia, 37007-Salamanca, Spain. olmo@usal.es
authors.forename: Esther
authors.initials: E
authors.lastname: del Olmo
authors.forename: Marlon García
authors.initials: MG
authors.lastname: Armas
authors.forename: MaInés
authors.initials: M
authors.lastname: Ybarra
authors.forename: Josè Luis
authors.initials: JL
authors.lastname: López
authors.forename: Patricia
authors.initials: P
authors.lastname: Oporto
authors.forename: Alberto
authors.initials: A
authors.lastname: Giménez
authors.forename: Eric
authors.initials: E
authors.lastname: Deharo
authors.forename: Arturo
authors.initials: A
authors.lastname: San Feliciano
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D007093:Imidazoles; D007211:Indoles; D002738:Chloroquine