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Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11?-HSD1 Inhibitors.


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 11?-HSD1. In continuation of our efforts to discover potent and selective 11?-HSD1 inhibitors, herein we explored several replacements for the cyclohexane ring. Some derivatives exhibited potent inhibitory activity against human 11?-HSD1, although with low selectivity over the isoenzyme 11?-HSD2, and poor microsomal stability.

SUBMITTER: Leiva R 

PROVIDER: S-EPMC6017749 | BioStudies | 2018-01-01T00:00:00Z

REPOSITORIES: biostudies

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