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Molecules 2009, 14(10), 4120-4135; doi:10.3390/molecules14104120

New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents

1,* , 1
2, 1, 1, 2, 2, 2, 1 and 1
1 Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain 2 Departamento de Parasitología, Facultad de Farmacia, Complutense University of Madrid, Spain
* Author to whom correspondence should be addressed.
Received: 11 August 2009 / Revised: 21 September 2009 / Accepted: 14 October 2009 / Published: 14 October 2009
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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 antimalarial agents; benzo[b]thiophene; 1-aryl-3-substituted propanol derivatives; P. Falciparum; ferriprotoporphyrin
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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