Nogal-Ruiz, J.J. (Juan J.)
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- New 1-aryl-3-substituted propanol derivatives as antimalarial agents(MDPI, 2009) Martinez-Fernandez, A.R. (Antonio R.); Martin-Perez-Solorzano, B. (Berta); Aldana, I. (Ignacio); Pérez-Silanes, S. (Silvia); Garcia–Sanchez, R.N. (Rory N.); Galiano, S. (Silvia); Monge, A. (Antonio); Berrade, L. (Luis); Mendoza, A. (Adela); Nogal-Ruiz, J.J. (Juan J.)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.