Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors

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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.date.updated2018-06-01T14:21:56Z
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.identifier.idgrec679150
dc.identifier.issn1420-3049
dc.identifier.pmid29495550
dc.identifier.urihttps://hdl.handle.net/2445/122728
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.accessRightsinfo:eu-repo/semantics/openAccess
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

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