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

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RECERCAT Home > Universitat de Barcelona > Farmacologia, Toxicologia i Química Terapèutica > Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) > View document

To access the full text documents, please follow this link: http://hdl.handle.net/2445/122728

dc.contributor	Universitat de Barcelona
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	2018-06-01T14:21:56Z
dc.date	2018-06-01T14:21:56Z
dc.date	2018-02-28
dc.date	2018-06-01T14:21:56Z
dc.identifier.citation	1420-3049
dc.identifier.citation	679150
dc.identifier.uri	http://hdl.handle.net/2445/122728
dc.format	14 p.
dc.format	application/pdf
dc.language.iso	eng
dc.publisher	MDPI
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	info:eu-repo/semantics/openAccess
dc.rights	http://creativecommons.org/licenses/by/3.0/es
dc.subject	Disseny de medicaments
dc.subject	Química farmacèutica
dc.subject	Enzims
dc.subject	Compostos policíclics
dc.subject	Drug design
dc.subject	Pharmaceutical chemistry
dc.subject	Enzymes
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
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.

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