| Author | Siqueira Filho, Ezequias Pessoa | |
| Author | Cerávolo, Isabela Penna | |
| Author | Kohlhoff, Markus | |
| Author | Krettli, Antoniana Ursine | |
| Author | Zani, Carlos Leomar | |
| Access date | 2018-08-24T13:11:10Z | |
| Available date | 2018-08-24T13:11:10Z | |
| Document date | 2018 | |
| Citation | SIQUEIRA FILHO, Ezequias Pessoa et al. Synthesis and Antiplasmodial Activity of 2-Methyl-3- Carboxyl-Naphtho [2, 3-B] Furan Quinone Derivatives. Journal of Medicinal Chemistry and Drug Design, v. 1, n. 2, p. 1-8, 2018. | pt_BR |
| ISSN | 2578-9589 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/28349 | |
| Language | eng | pt_BR |
| Publisher | Science Publishing Group | pt_BR |
| Rights | open access | pt_BR |
| Subject in Portuguese | Quinonas de naftofurano | pt_BR |
| Subject in Portuguese | Plasmodium falciparum | pt_BR |
| Subject in Portuguese | Malaria | pt_BR |
| Subject in Portuguese | Descoberta de drogas | pt_BR |
| Title | Synthesis and Antiplasmodial Activity of 2-Methyl-3- Carboxyl-Naphtho [2, 3-B] Furan Quinone Derivatives | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.16966/2578-9589.108 | |
| Abstract | Malaria, a disease caused by the Plasmodium parasite, has spread globally, mainly in the African subcontinent. Species of parasites resistant to usual drugs like chloroquine, used to treat malaria, have led research groups to search for new drugs to expand the current therapeutic arsenal. Fourteen 2-methyl-3-carboxylnaphtho[2,3-b]furan quinone derivatives (FNQ) were synthesized and evaluated using cultures of Plasmodium falciparum in vitro. From all FNQ derivatives tested, six of them (4,7-10,14) showed
IC50 values ranging from 0.05 μM to 11.3 μM. The glutamine-FNQ (9) and spermidine-FNQ derivatives (14) were the best antiplasmodial molecules tested, with selectivity indexes of 56 and 75, respectively. Our data suggests these two compounds are appropriate candidates for investigation as potential antimalarial drugs against drug-resistant Plasmodium species. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Química de Produtos Naturais Bioativos. Belo Horizonte MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Malária Experimental e Humana. Belo Horizonte MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Química de Produtos Naturais Bioativos. Belo Horizonte MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Malária Experimental e Humana. Belo Horizonte MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto René Rachou. Laboratório de Química de Produtos Naturais Bioativos. Belo Horizonte MG, Brasil. | pt_BR |
| Subject | Naphthofuran quinones | pt_BR |
| Subject | Plasmodium falciparum | pt_BR |
| Subject | Malaria | pt_BR |
| Subject | Drug Discovery | pt_BR |
