Leiva Martínez, RosanaMcBride, AndrewBinnie, MargaretWebster, Scott P.Vázquez Cruz, Santiago2018-06-012018-06-012018-02-281420-3049https://hdl.handle.net/2445/122728We 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.14 p.application/pdfengcc-by (c) Leiva Martínez, Rosana et al., 2018http://creativecommons.org/licenses/by/3.0/esDisseny de medicamentsQuímica farmacèuticaEnzimsCompostos policíclicsDrug designPharmaceutical chemistryEnzymesPolycyclic compoundsinfo:eu-repo/semantics/article6791502018-06-01info:eu-repo/semantics/openAccess29495550