title: New 1-aryl-3-substituted propanol derivatives as antimalarial agents.
abstract: This paper describes the synthesis and in vitro antimalarial activity against a P. falciparum 3D7 strain of some new 1-aryl-3-substituted propanol derivatives. Twelve of the tested compounds showed an IC(50) lower than 1 microM. These compounds were also tested for cytotoxicity in murine J774 macrophages. The most active compounds were evaluated for in vivo activity against P. berghei in a 4-day suppressive test. Compound 12 inhibited more than 50% of parasite growth at a dose of 50 mg/kg/day. In addition, an FBIT test was performed to measure the ability to inhibit ferriprotoporphyrin biocrystallization. This data indicates that 1-aryl-3-substituted propanol derivatives hold promise as a new therapeutic option for the treatment of malaria.
authors.affiliation: Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada, University of Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain. sperez@unav.es
authors.forename: Silvia
authors.initials: S
authors.lastname: Pérez-Silanes
authors.forename: Luis
authors.initials: L
authors.lastname: Berrade
authors.forename: Rory N
authors.initials: RN
authors.lastname: García-Sánchez
authors.forename: Adela
authors.initials: A
authors.lastname: Mendoza
authors.forename: Silvia
authors.initials: S
authors.lastname: Galiano
authors.forename: Berta Martín
authors.initials: BM
authors.lastname: Pérez-Solórzano
authors.forename: Juan J
authors.initials: JJ
authors.lastname: Nogal-Ruiz
authors.forename: Antonio R
authors.initials: AR
authors.lastname: Martínez-Fernández
authors.forename: Ignacio
authors.initials: I
authors.lastname: Aldana
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D020128:Inhibitory Concentration 50; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects*; D010963:Plasmodium falciparum / Q000187:drug effects*; D020005:Propanols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D020005:Propanols