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

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....

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Bibliographic Details
Main Authors: Antonio Monge, Ignacio Aldana, Juan J. Nogal-Ruiz, Antonio R. Martínez-Fernández, Berta Martín Pérez-Solórzano, Silvia Galiano, Adela Mendoza, Silvia Pérez-Silanes, Luis Berrade, Rory N. García–Sánchez
Format: Article
Language:English
Published: MDPI AG 2009-10-01
Series:Molecules
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Online Access:http://www.mdpi.com/1420-3049/14/10/4120/
Description
Summary: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.
ISSN:1420-3049