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

Molecules

Silvia Pérez-Silanes¹  Luis Berrade¹  Rory N. García–Sánchez¹  Adela Mendoza¹  Silvia Galiano¹  Berta Martín Pérez-Solórzano¹  Juan J. Nogal-Ruiz¹  Antonio R. Martínez-Fernández¹  Ignacio Aldana¹ 

[1] ¹Unidad en Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, c/Irunlarrea s/n, 31080 Pamplona, Spain ²Departamento de Parasitología, Facultad de Farmacia, Complutense University of Madrid, Spain

关键词: antimalarial agents;    benzo[b]thiophene;    1-aryl-3-substituted propanol derivatives;    P. Falciparum;    ferriprotoporphyrin;   

DOI  :  10.3390/molecules14104120

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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.