Exploring N-acyl-4-azatetracyclo[5.3.2.0 2,6 .0 8,10 ]dodec-11-enes as 11β-HSD1 Inhibitors
We recently found that a cyclohexanecarboxamide derived from 4-azatetracyclo[5.3.2.0 .0 ]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....
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Veröffentlicht in: | Molecules (Basel, Switzerland) Switzerland), 2018-02, Vol.23 (3), p.536 |
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Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | We recently found that a cyclohexanecarboxamide derived from 4-azatetracyclo[5.3.2.0
.0
]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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ISSN: | 1420-3049 1420-3049 |
DOI: | 10.3390/molecules23030536 |