Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/6742

Type
Article
Copyright
Restricted access
Collections
Share

Statistics
Metadata
Show full item record

ANTIMALARIAL ACTIVITY OF 4-(5-TRIFLUOROMETHYL-1H-PYRAZOL-1-YL)-CHLOROQUINE ANALOGUES
Cunico, Wilson et al. | Date Issued: 2006
Author
Cunico, Wilson
Cechinel, Cleber A.
Bonacorso, Helio G.
Martins, Marcos Antonio Pinto
Zanatta, Nilo
Souza, Marcus Vinícius Nora de
Freitas, Isabela O.
Soares, Rodrigo Pedro Pinto
Krettli, Antoniana Ursine
Affilliation
Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil.
Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil.
Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil.
Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil.
Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil.
Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil.
Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil.
Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil.
Abstract
The antimalarial activity of chloroquine-pyrazole analogues, synthesized from the reaction of 1,1,1-trifluoro-4-methoxy-3-alken-2-ones with 4-hydrazino-7-chloroquinoline, has been evaluated in vitro against a chloroquine resistant Plasmodium falciparumclone. Parasite growth in the presence of the test drugs was measured by incorporation of [3H] hypoxanthine in compar-ison to controls with no drugs. All but one of the eight (4,5-dihydropyrazol-1-yl) chloroquine 2derivatives tested showed a significant activity in vitro, thus, are a promising new class of antimalarials. The three most active ones were also tested in vivo against Plasmodium bergheiin mice. However, the (pyrazol-1-yl) chloroquine 3derivatives were mostly inactive, suggesting that the aromatic functionality of the pyrazole ring was critical
Keywords
Antimalarials/pharmacology
Chloroquine/analogs & derivatives
Dose-Response Relationship, Drug Humans
Plasmodium falciparum/drug effects
 
Citation
CUNICO, Wilson et al. Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)-chloroquine analogues. Bioorg Med Chem Lett., v. 16, n. 3, p. 649-653, Feb. 2006.