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- Title
Exploring N-acyl-4-azatetracyclo[5.3.2.0<sup>2,6</sup>.0<sup>8,10</sup>]dodec-11-enes as 11β-HSD1 Inhibitors.
- Authors
Leiva, Rosana; McBride, Andrew; Binnie, Margaret; Webster, Scott P.; Vázquez, Santiago
- 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.
- Subjects
CYCLOHEXANE derivatives; CARBOXAMIDES; DRUG development; ENZYME inhibitors synthesis; THERAPEUTIC use of glucocorticoids; NEUROPROTECTIVE agents; ALZHEIMER'S disease treatment
- Publication
Molecules, 2018, Vol 23, Issue 3, p536
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules23030536