Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors

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Title:	Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors
Author:	Leiva Martínez, Rosana; McBride, Andrew; Binnie, Margaret; Webster, Scott P.; Vázquez Cruz, Santiago
Other authors:	Universitat de Barcelona
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.
Subject(s):	-Disseny de medicaments -Química farmacèutica -Enzims -Compostos policíclics -Drug design -Pharmaceutical chemistry -Enzymes -Polycyclic compounds
Rights:	cc-by (c) Leiva Martínez, Rosana et al., 2018 http://creativecommons.org/licenses/by/3.0/es
Document type:	Article Article - Published version
Published by:	MDPI
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