| Author | Bernardino, Alice M. R. | |
| Author | Gomes, Adriana O. | |
| Author | Charret, Karen S. | |
| Author | Freitas, Antônio C. C. | |
| Author | Machado, Gérzia M. C. | |
| Author | Cavalheiro, Marilene M. Canto | |
| Author | Leon, Leonor L. | |
| Author | Amaral, Veronica F. | |
| Access date | 2019-12-31T20:29:34Z | |
| Available date | 2019-12-31T20:29:34Z | |
| Document date | 2006 | |
| Citation | BERNARDINO, Alice M. R. et al. Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N′-[(4-Y-phenyl)methylene]-1H-pyrazole-4-carbohydrazides. European Journal of Medicinal Chemistry, v. 41, p. 80-87, Jan. 2006. | pt_BR |
| ISSN | 0223-5234 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/38920 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Síntese | pt_BR |
| Subject in Portuguese | Atividade antileishmanial | pt_BR |
| Subject in Portuguese | Citotoxicidade | pt_BR |
| Title | Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N'-[(4-Y-phenyl)methylene]-1H-pyrazole-4-carbohydrazides | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.ejmech.2005.10.007 | |
| Abstract | 1H-pyrazole-4-carbohydrazides were synthesized and their leishmanicidal in vitro activities and cytotoxic effects were investigated. The drugs prototypes of these new compounds (ketoconazole, benznidazole, allopurinol and pentamidine) were also tested. It was found that among all the 1H-pyrazole-4-carbohydrazides derivatives examined, the most active compounds were those with X = Br, Y = NO2 (27) and X = NO2, Y = Cl (15) derivatives which showed to be most effective on promastigotes forms of L. amazonensis than on L. chagasi and L. braziliensis species. When tested against murine peritoneal macrophages as mammalian host cell controls of toxicity, 1-(4-Br-phenyl)-N'-[(4-NO(2)-phenyl)methylene]-1H-pyrazole-4-carbohydrazides (27) (EC50 = 50 microM l(-1)) and 1-(4-NO2-phenyl)-N'-[(4-Cl-phenyl)methylene]-1H-pyrazole-4-carbohydrazides (15) EC50 = 80 microM l(-1))] was reasonably toxic. However, both compounds were less toxic than pentamidine and ketoconazole. These results provide new perspectives on the development of drugs with activities against Leishmania parasite. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Programa de Pós-Grduação em Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Química. Departamento de Química Orgânica. Programa de Pós-Grduação em Química Orgânica. Niterói, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Imunobiologia. Niterói, RJ, Brasil.. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Faculdade de Farmácia. Niterói, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunobiologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunobiologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunobiologia. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal Fluminense. Instituto de Biologia. Departamento de Imunobiologia. Niterói, RJ, Brasil.. | pt_BR |
| Subject | Synthesis | pt_BR |
| Subject | Antileishmania activity | pt_BR |
| Subject | Cytotoxicity | pt_BR |
| e-ISSN | 1768-3254 | |
| Embargo date | 2030-12-31 | |
