Artículo
Novel sulfamides and sulfamates derived from amino esters: Synthetic studies and anticonvulsant activity
Villalba, Maria Luisa
; Enrique, Andrea Verónica
; Higgs, Josefina
; Castaño, Rocío A.; Goicoechea, Sofia; Taborda, Facundo; Gavernet, Luciana
; Lick, Ileana Daniela
; Marder, Nora Mariel
; Bruno Blanch, Luis Enrique
Fecha de publicación:
03/2016
Editorial:
Elsevier Science
Revista:
European Journal of Pharmacology
ISSN:
0014-2999
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
We report herein the design and optimization of a novel series of sulfamides and sulfamates derived from amino esters with anticonvulsant properties. The structures were designed based on the pharmacophoric pattern previously proposed, with the aim of improving the anticonvulsant action. The compounds were obtained by a new synthetic procedure with microwave assisted heating and the use of adsorbents in the isolation process. All the derivatives showed protection against the maximal electroshock seizure test (MES test) in mice at the lowest dose tested (30 mg/kg) but they did not show significant protection against the chemical induced convulsion by pentylenetetrazole. These results verify the ability of the computational model for designing new anticonvulsants structures with anti-MES activity. Additionally, we evaluated the capacity of the synthesized structures to bind to the benzodiazepine binding site (BDZ-bs) of the γ-aminobutiric acid receptor (GABAA receptor). Some of them showed medium to low affinity for the BDZ-bs.
Palabras clave:
Epilepsy
,
Sulfamides
,
Sulfamates
,
Synthesis
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Articulos(CCT - LA PLATA)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - LA PLATA
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - LA PLATA
Articulos(CINDECA)
Articulos de CENTRO DE INV EN CS.APLICADAS "DR.JORGE J.RONCO"
Articulos de CENTRO DE INV EN CS.APLICADAS "DR.JORGE J.RONCO"
Articulos(IQUIFIB)
Articulos de INST.DE QUIMICA Y FISICO-QUIMICA BIOLOGICAS "PROF. ALEJANDRO C. PALADINI"
Articulos de INST.DE QUIMICA Y FISICO-QUIMICA BIOLOGICAS "PROF. ALEJANDRO C. PALADINI"
Citación
Villalba, Maria Luisa; Enrique, Andrea Verónica; Higgs, Josefina; Castaño, Rocío A.; Goicoechea, Sofia; et al.; Novel sulfamides and sulfamates derived from amino esters: Synthetic studies and anticonvulsant activity; Elsevier Science; European Journal of Pharmacology; 774; 3-2016; 55-63
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