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New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents
Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain
Departamento de Parasitología, Facultad de Farmacia, Complutense University of Madrid, Spain
* Author to whom correspondence should be addressed.
Received: 11 August 2009; in revised form: 21 September 2009 / Accepted: 14 October 2009 / Published: 14 October 2009
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.
Keywords: antimalarial agents; benzo[b]thiophene; 1-aryl-3-substituted propanol derivatives; P. Falciparum; ferriprotoporphyrin
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MDPI and ACS Style
Pérez-Silanes, S.; Berrade, L.; García–Sánchez, R.N.; Mendoza, A.; Galiano, S.; Pérez-Solórzano, B.M.; Nogal-Ruiz, J.J.; Martínez-Fernández, A.R.; Aldana, I.; Monge, A. New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents. Molecules 2009, 14, 4120-4135.
Pérez-Silanes S, Berrade L, García–Sánchez RN, Mendoza A, Galiano S, Pérez-Solórzano BM, Nogal-Ruiz JJ, Martínez-Fernández AR, Aldana I, Monge A. New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents. Molecules. 2009; 14(10):4120-4135.
Pérez-Silanes, Silvia; Berrade, Luis; García–Sánchez, Rory N.; Mendoza, Adela; Galiano, Silvia; Pérez-Solórzano, Berta M.; Nogal-Ruiz, Juan J.; Martínez-Fernández, Antonio R.; Aldana, Ignacio; Monge, Antonio. 2009. "New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents." Molecules 14, no. 10: 4120-4135.