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
Hauptverfasser: Leiva, Rosana, McBride, Andrew, Binnie, Margaret, Webster, Scott P, Vázquez, Santiago
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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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules23030536