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Dadun > Depósito Académico > CIFA (Centro de Investigación en Farmacobiología Aplicada) > Unidad de I+D de Medicamentos > DA - CIFA - I+D de medicamentos - Artículos de revistas >

New 1-aryl-3-substituted propanol derivatives as antimalarial agents
Authors: Perez-Silanes, S. (Silvia)
Berrade, L. (Luis)
Garcia–Sanchez, R.N. (Rory N.)
Mendoza, A. (Adela)
Galiano, S. (Silvia)
Martin-Perez-Solorzano, B. (Berta)
Nogal-Ruiz, J.J. (Juan J.)
Martinez-Fernandez, A.R. (Antonio R.)
Aldana, I. (Ignacio)
Monge, A. (Antonio)
Keywords: Antimalarial agents
Benzo(b)thiophene
1-aryl-3-substituted propanol derivatives
P. Falciparum
Ferriprotoporphyrin
Issue Date: 2009
Publisher: MDPI
Publisher version: http://www.mdpi.com/journal/molecules
ISSN: 1420-3049
Citation: Perez-Silanes S, Berrade L, Garcia-Sanchez RN, Mendoza A, Galiano S, Perez-Solorzano BM, et al. New 1-aryl-3-substituted propanol derivatives as antimalarial agents. Molecules 2009 Oct 14;14(10):4120-4135.
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 IC50 lower than 1 μM. 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.
Permanent link: http://hdl.handle.net/10171/23600
Appears in Collections:DA - Farmacia - Orgánica - Artículos de revista
DA - CIFA - I+D de medicamentos - Artículos de revistas

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