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http://hdl.handle.net/10261/9506
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Campo DC | Valor | Lengua/Idioma |
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dc.contributor.author | Serrano, Pedro | - |
dc.contributor.author | Casas, Josefina | - |
dc.contributor.author | Zucco, Martine | - |
dc.contributor.author | Emeric, Gilbert | - |
dc.contributor.author | Egido-Gabás, Meritxell | - |
dc.contributor.author | Llebaria, Amadeu | - |
dc.contributor.author | Delgado Huertas, Antonio | - |
dc.date.accessioned | 2009-01-09T11:22:26Z | - |
dc.date.available | 2009-01-09T11:22:26Z | - |
dc.date.issued | 2007-11-18 | - |
dc.identifier.citation | Journal of Combinatorial Chemistry 9(1): 43-52 (2007) | en_US |
dc.identifier.issn | 1520-4774 | - |
dc.identifier.uri | http://hdl.handle.net/10261/9506 | - |
dc.description | 9 pages, 8 figuras.-- PMID: 17206831 [PubMed].-- Supporting information (31 pages) available at: http://pubs.acs.org/doi/suppl/10.1021/cc060080o/suppl_file/cc060080osi20060615_053230.pdf | en_US |
dc.description.abstract | Libraries of N-substituted aminocyclitol derivatives of the scyllo and racemic chiro series by means of parallel solution-phase methodology with the help of robotic technology are described. Chemical diversity has been introduced by reaction of selected scaffolds with a set of aldehydes, acyl chlorides, sulfonyl chlorides, chloroformates, and amines to afford the corresponding amines, amides, sulfonamides, carbamates and ureas, respectively. The optimized methodology has proven excellent, in terms of overall purities of the resulting libraries, for the production of amides. Sulfonamides and carbamates have been obtained in slightly lower purities, while amines afforded modest results. Selected library members have been evaluated as inhibitors of recombinant glucocerebrosidase with K(i) values ranging in the low micromolar scale for the most active members. | en_US |
dc.description.sponsorship | Partial financial support from Ministerio de Ciencia y Tecnología (Spain) (Projects MCYT BQU2002-03737 and CTQ2005-00175/BQU), Fondos Feder (EU), Ministerio de Sanidad y Consumo, Spain (Project FIS, PIO40767), CSIC (Project 2004-80F026), and Generalitat de Catalunya (Projects 2005SGR01063) is acknowledged. P.S. and M.E.-G. thank Spanish "Ministerio de Educación y Cultura” and CSIC, respectively, for predoctoral fellowships. The authors also thank Genzyme for a generous gift of Imiglucerase (Cerezyme) and Mrs. Mireia Garrido for experimental contributions. | en_US |
dc.format.extent | 162 bytes | - |
dc.format.mimetype | application/msword | - |
dc.language.iso | eng | en_US |
dc.publisher | American Chemical Society | en_US |
dc.rights | closedAccess | en_US |
dc.subject | N-Aminocyclitol libraries | en_US |
dc.subject | Glucocerebrosidase inhibitors | en_US |
dc.subject | Amides | en_US |
dc.subject | Sulfonamides | en_US |
dc.subject | Carbamates | en_US |
dc.title | Combinatorial approach to N-substituted aminocyclitol libraries by solution-phase parallel synthesis and preliminary evaluation as glucocerebrosidase inhibitors | en_US |
dc.type | artículo | en_US |
dc.identifier.doi | 10.1021/cc060080o | - |
dc.description.peerreviewed | Peer reviewed | en_US |
dc.relation.publisherversion | http://dx.doi.org/10.1021/cc060080o | en_US |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.languageiso639-1 | en | - |
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