Synthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp

dc.creatorFaria, Jéssica V.
dc.creatorSantos, Maurício S. dos
dc.creatorBernardino, Alice M. R.
dc.creatorBecker, Klaus M.
dc.creatorMachado, Gérzia M. C.
dc.creatorRodrigues, Raquel F.
dc.creatorCavalheiro, Marilene M. Canto
dc.creatorLeon, Leonor L.
dc.date2016-08-25T13:47:53Z
dc.date2016-08-25T13:47:53Z
dc.date2013
dc.date.accessioned2023-09-26T21:10:34Z
dc.date.available2023-09-26T21:10:34Z
dc.identifierFARIA, Jéssica V. et al. Synthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp. Bioorganic & Medicinal Chemistry Letters, v.23, n.23, p.6310-6312, Dec. 2013.
dc.identifier0960-894X
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/15393
dc.identifier10.1016/j.bmcl.2013.09.062
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8870352
dc.descriptionA new series of 5-(1-aryl-3-methyl-1H-pyrazol-4-yl)-1H-tetrazole derivatives (4a-m) and their precursor 1-aryl-3-methyl-1H-pyrazole-4-carbonitriles (3a-m) were synthesized and evaluated as antileishmanials against Leishmania braziliensis and Leishmania amazonensis promastigotes in vitro. In parallel, the cytotoxicity of these compounds was evaluated on the RAW 264.7 cell line. The results showed that among the assayed compounds the substituted 3-chlorophenyl (4a) (IC50/24h=15±0.14 μM) and 3,4-dichlorophenyl tetrazoles (4d) (IC50/24h=26±0.09 μM) were the most potent against L. braziliensis promastigotes, as compared the reference drug pentamidine, which presented IC50=13±0.04 μM. In addition, 4a and 4d derivatives were less cytotoxic than pentamidine. However, these tetrazole derivatives (4) and pyrazole-4-carbonitriles precursors (3) differ against each of the tested species and were more effective against L.braziliensis than on L. amazonensis.
dc.description2030-01-01
dc.formatapplication/pdf
dc.languageeng
dc.publisherScienceDirect
dc.rightsrestricted access
dc.subjectLeishmania braziliensis
dc.subjectAtividade leishmanicida
dc.subjectTetrazole
dc.subjectAntileishmanial activity
dc.subjectLeishmania braziliensis
dc.subjectLeishmania amazonensis
dc.subjectTetrazole
dc.titleSynthesis and activity of novel tetrazole compounds and their pyrazole-4-carbonitrile precursors against Leishmania spp
dc.typeArticle


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