Synthesis and leishmanicidal activities of 1-(4-X-phenyl)-N'-[(4-Y-phenyl)methylene]-1H-pyrazole-4-carbohydrazides

dc.creatorBernardino, Alice M. R.
dc.creatorGomes, Adriana O.
dc.creatorCharret, Karen S.
dc.creatorFreitas, Antônio C. C.
dc.creatorMachado, Gérzia M. C.
dc.creatorCavalheiro, Marilene M. Canto
dc.creatorLeon, Leonor L.
dc.creatorAmaral, Veronica F.
dc.date2019-12-31T20:29:34Z
dc.date2019-12-31T20:29:34Z
dc.date2006
dc.date.accessioned2023-09-26T22:40:36Z
dc.date.available2023-09-26T22:40:36Z
dc.identifierBERNARDINO, 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, 2006.
dc.identifier0223-5234
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/38920
dc.identifier10.1016/j.ejmech.2005.10.007
dc.identifier1768-3254
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8881804
dc.description1H-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.
dc.description2025-01-01
dc.formatapplication/pdf
dc.languageeng
dc.publisherElsevier
dc.rightsrestricted access
dc.subjectSíntese
dc.subjectAtividade antileishmanial
dc.subjectCitotoxicidade
dc.subjectSynthesis
dc.subject1-(4-X-phenyl)-N′-[(4-Y-phenyl)methylene]-1H-pyrazole-4-carbohydrazides
dc.subjectAntileishmania activity
dc.subjectCytotoxicity
dc.titleSynthesis and leishmanicidal activities of 1-(4-X-phenyl)-N'-[(4-Y-phenyl)methylene]-1H-pyrazole-4-carbohydrazides
dc.typeArticle


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