Exploring N-acyl-4-azatetracyclo[5.3.2.0.0]dodec-11-enes as 11β-HSD1 Inhibitors

Rosana Leiva, Andrew McBride, Margaret Binnie, Scott P Webster, Santiago Vázquez

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
JournalMolecules
Volume23
Issue number3
DOIs
Publication statusPublished - 28 Feb 2018

Keywords

  • Journal Article

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