| Author | Cunico, Wilson | |
| Author | Cechinel, Cleber A. | |
| Author | Bonacorso, Helio G. | |
| Author | Martins, Marcos Antonio Pinto | |
| Author | Zanatta, Nilo | |
| Author | Souza, Marcus Vinícius Nora de | |
| Author | Freitas, Isabela O. | |
| Author | Soares, Rodrigo Pedro Pinto | |
| Author | Krettli, Antoniana Ursine | |
| Access date | 2013-08-05T13:38:51Z | |
| Available date | 2013-08-05T13:38:51Z | |
| Document date | 2006 | |
| 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. | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/6742 | |
| Language | eng | pt_BR |
| Rights | restricted access | pt_BR |
| Title | Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)-chloroquine analogues | pt_BR |
| Type | Article | |
| 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 | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Santa Maria. Departamento de Química. Núcleo de Química de Heterociclos. Santa Maria, RS, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisas Rene Rachou. Belo Horizonte, MG, Brasil / Universidade Federal de Minas Gerais. Departamento de Parasitologia. Belo Horizonte, MG, Brasil. | pt_BR |
| Subject | Antimalarials/pharmacology | pt_BR |
| Subject | Chloroquine/analogs & derivatives | pt_BR |
| Subject | Dose-Response Relationship, Drug Humans | pt_BR |
| Subject | Plasmodium falciparum/drug effects | pt_BR |
