New 1-aryl-3-substituted propanol derivatives as antimalarial agents.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Silvia Pérez-SilanesAntonio Monge

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 IC(50) lower than 1 microM. 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.

Citations

Nov 12, 2013·European Journal of Medicinal Chemistry·Pedro M García-BarrantesArturo San Feliciano
Oct 23, 2016·International Journal for Parasitology. Drugs and Drug Resistance·Miguel QuilianoSilvia Galiano
Jan 13, 2012·Beilstein Journal of Organic Chemistry·Matthias D'hoogheNorbert De Kimpe
Mar 2, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jelena KonstantinovićBogdan Šolaja
Dec 23, 2016·Journal of Medicinal Chemistry·Elsa Moreno-ViguriSilvia Pérez-Silanes

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Methods Mentioned

BETA
acylation
nuclear magnetic resonance
column flash
column chromatography

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Antimalarial Agents (ASM)

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.

Antimalarial Agents

Antimalarial agents, also known as antimalarials, are designed to prevent or cure malaria. Discover the latest research on antimalarial agents here.