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- Title
New 1-Aryl-3-Substituted Propanol Derivatives as Antimalarial Agents.
- Authors
Pérez-Silanes, Silvia; Berrade, Luis; GarcíaSánchez, Rory N.; Mendoza, Adela; Galiano, Silvia; Pérez-Solórzano, Berta Martín; Nogal-Ruiz, Juan J.; Martínez-Fernández, Antonio R.; Aldana, Ignacio; Monge, Antonio
- 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.
- Subjects
PROPANOLS; MALARIA treatment; ANTIMALARIALS; PLASMODIUM falciparum; ORGANIC synthesis; LABORATORY rats; MACROPHAGES; CRYSTALLIZATION; BIOCHEMISTRY; THERAPEUTICS
- Publication
Molecules, 2009, Vol 14, Issue 10, p4120
- ISSN
1420-3049
- Publication type
Academic Journal
- DOI
10.3390/molecules14104120