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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/122728
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dc.contributor.authorLeiva Martínez, Rosana-
dc.contributor.authorMcBride, Andrew-
dc.contributor.authorBinnie, Margaret-
dc.contributor.authorWebster, Scott P.-
dc.contributor.authorVázquez Cruz, Santiago-
dc.date.accessioned2018-06-01T14:21:56Z-
dc.date.available2018-06-01T14:21:56Z-
dc.date.issued2018-02-28-
dc.identifier.issn1420-3049-
dc.identifier.urihttps://hdl.handle.net/2445/122728-
dc.description.abstractWe recently found that a cyclohexanecarboxamide derived from 4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene displayed low nanomolar inhibition of 11β-HSD1. In continuation of our efforts to discover potent and selective 11β-HSD1 inhibitors, herein we explored several replacements for the cyclohexane ring. Some derivatives exhibited potent inhibitory activity against human 11β-HSD1, although with low selectivity over the isoenzyme 11β-HSD2, and poor microsomal stability.-
dc.format.extent14 p.-
dc.format.mimetypeapplication/pdf-
dc.language.isoeng-
dc.publisherMDPI-
dc.relation.isformatofReproducció del document publicat a: https://doi.org/10.3390/molecules23030536-
dc.relation.ispartofMolecules, 2018, vol. 23, num. 3, p. E536-
dc.relation.urihttps://doi.org/10.3390/molecules23030536-
dc.rightscc-by (c) Leiva Martínez, Rosana et al., 2018-
dc.rights.urihttp://creativecommons.org/licenses/by/3.0/es-
dc.sourceArticles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)-
dc.subject.classificationDisseny de medicaments-
dc.subject.classificationQuímica farmacèutica-
dc.subject.classificationEnzims-
dc.subject.classificationCompostos policíclics-
dc.subject.otherDrug design-
dc.subject.otherPharmaceutical chemistry-
dc.subject.otherEnzymes-
dc.subject.otherPolycyclic compounds-
dc.titleExploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors-
dc.typeinfo:eu-repo/semantics/article-
dc.typeinfo:eu-repo/semantics/publishedVersion-
dc.identifier.idgrec679150-
dc.date.updated2018-06-01T14:21:56Z-
dc.rights.accessRightsinfo:eu-repo/semantics/openAccess-
dc.identifier.pmid29495550-
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Biomedicina (IBUB))

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