dc.contributor.author
Leiva Martínez, Rosana
dc.contributor.author
McBride, Andrew
dc.contributor.author
Binnie, Margaret
dc.contributor.author
Webster, Scott P.
dc.contributor.author
Vázquez Cruz, Santiago
dc.date.issued
2018-06-01T14:21:56Z
dc.date.issued
2018-06-01T14:21:56Z
dc.date.issued
2018-02-28
dc.date.issued
2018-06-01T14:21:56Z
dc.identifier
https://hdl.handle.net/2445/122728
dc.description.abstract
We 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
application/pdf
dc.relation
Reproducció del document publicat a: https://doi.org/10.3390/molecules23030536
dc.relation
Molecules, 2018, vol. 23, num. 3, p. E536
dc.relation
https://doi.org/10.3390/molecules23030536
dc.rights
cc-by (c) Leiva Martínez, Rosana et al., 2018
dc.rights
http://creativecommons.org/licenses/by/3.0/es
dc.rights
info:eu-repo/semantics/openAccess
dc.source
Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
dc.subject
Disseny de medicaments
dc.subject
Química farmacèutica
dc.subject
Compostos policíclics
dc.subject
Pharmaceutical chemistry
dc.subject
Polycyclic compounds
dc.title
Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors
dc.type
info:eu-repo/semantics/article
dc.type
info:eu-repo/semantics/publishedVersion
