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Do Carmo D.F.M.,Federal University of Amazonas | Amaral A.C.F.,Laboratorio Of Plantas Medicinais E Derivados | MacHado G.M.C.,Laboratorio Of Bioquimica Of Tripanosomatideos | Leon L.L.,Laboratorio Of Bioquimica Of Tripanosomatideos | De Andrade Silva J.R.,Federal University of Amazonas
Molecules | Year: 2012

The essential oils obtained from leaves of Piper duckei and Piper demeraranum by hydrodistillation were analyzed by gas chromatography-mass spectrometry. The main constituents found in P. demeraranum oil were limonene (19.3%) and β-elemene (33.1%) and in P. duckei oil the major components found were germacrene D (14.7%) and trans-caryophyllene (27.1%). P. demeraranum and P. duckei oils exhibited biological activity, with IC 50 values between 15 to 76 μg mL -1 against two Leishmania species, P. duckei oil being the most active. The cytotoxicity of the essential oils on mice peritoneal macrophage cells was insignificant, compared with the toxicity of pentamidine. The main mono- and sesquiterpene, limonene (IC 50 = 278 μM) and caryophyllene (IC 50 = 96 μM), were tested against the strains of Leishmania amazonensis, and the IC 50 values of these compounds were lower than those found for the essential oils of the Piper species. The HET-CAM test was used to evaluate the irritation potential of these oils as topical products, showing that these oils can be used as auxiliary medication in cases of cutaneous leishmaniasis, with less side effects and lower costs. Source


Dos Santos M.S.,Federal University of Itajuba | Bernardino A.M.R.,Federal University of Fluminense | Pinheiro L.C.S.,Federal University of Fluminense | Canto-Cavalheiro M.M.,Laboratorio Of Bioquimica Of Tripanosomatideos | Leon L.L.,Laboratorio Of Bioquimica Of Tripanosomatideos
Journal of Heterocyclic Chemistry | Year: 2012

A series of new 5-(1-aryl-1H-pyrazole-4-yl)-1H-tetrazoles 4a-l were synthesized via [3 + 2] cycloaddition reaction from 1-aryl-1H-pyrazole-4- carbonitriles 3a-l, sodium azide and ammonium chloride, using dimethylformamide (DMF) as solvent, in good yields: 64-85%. The structures of these newly synthesized compounds were determined from the IR, 1H- and 13C-NMR spectroscopic data and elemental analyses. © 2012 HeteroCorporation. Source


Dos Santos M.S.,Federal University of Itajuba | Oliveira M.L.V.,Federal University of Fluminense | Bernardino A.M.R.,Federal University of Fluminense | De Leo R.M.,Laboratorio Of Bioquimica Of Tripanosomatideos | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

A series of 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (4a-g) and 5-amino-1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-1H-pyrazoles (5a-g) were synthesized and evaluated in vitro against three Leishmania species: L. amazonensis, L. braziliensis and L. infantum (L. chagasi syn.). The cytotoxicity was assessed. Among the derivatives examined, six compounds emerged as the most active on promastigotes forms of L. amazonensis with IC50 values ranging from 15 to 60 μM. The reference drug pentamidine presented IC 50 = 10 μM. However, these new compounds were less cytotoxic than pentamidine. Based on these results, the more promising derivative 5d was tested further in vivo. This compound showed inhibition of the progression of cutaneous lesions in CBA mice infected with L. amazonensis relative to an untreated control. © 2011 Elsevier Ltd. All rights reserved. Source


Faria J.V.,Federal University of Fluminense | Dos Santos M.S.,Federal University of Itajuba | Bernardino A.M.R.,Federal University of Fluminense | Becker K.M.,Laboratorio Of Bioquimica Of Tripanosomatideos | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013

A 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) (IC50/24 h = 15 ± 0.14 μM) and 3,4-dichlorophenyl tetrazoles (4d) (IC50/24 h = 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. © 2013 Elsevier Ltd. All rights reserved. Source


Borges J.C.,Federal University of Fluminense | Carvalho A.V.,Laboratorio Of Bioquimica Of Tripanosomatideos | Bernardino A.M.R.,Federal University of Fluminense | Oliveira C.D.,Federal University of Fluminense | And 10 more authors.
Journal of the Brazilian Chemical Society | Year: 2014

This paper describes the synthesis and the antileishmanial activity of new pyrazolyl benzenesulfonamide derivatives. These were elucidated by spectrometric methods. Some compounds showed a significant in vitro activity against Leishmania amazonensis, highlighting the derivative 1e. These pyrazolyl benzenesulfonamide derivatives did not show any toxicity in murine macrophage. © 2014 Sociedade Brasileira de Química. Source

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