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dc.contributor.author
Villalba, Maria Luisa
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Palestro, Pablo Hernán
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Ceruso, Mariangela
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Talevi, Alan
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Gonzalez Funes, Jose L.
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Bruno Blanch, Luis Enrique
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Supuran, Claudiu T.
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Gavernet, Luciana
dc.date.available
2017-09-20T20:06:16Z
dc.date.issued
2016-02-15
dc.identifier.citation
Villalba, Maria Luisa; Palestro, Pablo Hernán; Ceruso, Mariangela; Talevi, Alan; Gonzalez Funes, Jose L.; et al.; Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action; Pergamon-Elsevier Science Ltd.; Bioorganic & Medicinal Chemistry; 24; 4; 15-2-2016; 894-901
dc.identifier.issn
0968-0896
dc.identifier.uri
http://hdl.handle.net/11336/24743
dc.description.abstract
A set of N,N0 -disubstituted sulfamides and sodium cyclamate have been tested for their inhibitory action against six isoforms of carbonic anhydrase (CA, EC 4.2.1.1) found in the brain, that is, CA I, CA II, CA VII, CA IX, CA XII and CA XIV, some of which are involved in epileptogenesis. The biological data showed interesting results for CA VII inhibition, the isozyme thought to be a novel antiepileptic target. Strong CA VII inhibitors, with Ki values in the low nanomolar–subnanomolar range were identified. Some of these derivatives showed selectivity for inhibition of CA VII versus the ubiquitous isoform CA II, for which the Ki values were in the micromolar range. Molecular modeling approaches were employed to understand the binding interactions between these compounds and the two CA isoforms, since the mechanism of action of such disubstituted sulfamides was not yet investigated by means of X-ray crystallography
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Pergamon-Elsevier Science Ltd.
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Carbonic Anhydrase
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Sulfamides
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Docking
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Epilepsy
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Sodium Cyclamate
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Bioquímica y Biología Molecular
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Ciencias Biológicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2017-09-19T14:17:44Z
dc.journal.volume
24
dc.journal.number
4
dc.journal.pagination
894-901
dc.journal.pais
Estados Unidos
dc.journal.ciudad
New York
dc.description.fil
Fil: Villalba, Maria Luisa. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina
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Fil: Palestro, Pablo Hernán. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
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Fil: Ceruso, Mariangela. Universita Degli Studi Di Firenze; Italia
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Fil: Talevi, Alan. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Gonzalez Funes, Jose L.. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina
dc.description.fil
Fil: Bruno Blanch, Luis Enrique. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Supuran, Claudiu T.. Universita Degli Studi Di Firenze; Italia
dc.description.fil
Fil: Gavernet, Luciana. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title
Bioorganic & Medicinal Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry/
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.bmc.2016.01.012
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