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http://hdl.handle.net/2445/122728| 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 |
| Keywords: | Disseny de medicaments Química farmacèutica Enzims Compostos policíclics Drug design Pharmaceutical chemistry Enzymes Polycyclic compounds |
| Issue Date: | 28-Feb-2018 |
| Publisher: | MDPI |
| 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. |
| Note: | Reproducció del document publicat a: https://doi.org/10.3390/molecules23030536 |
| It is part of: | Molecules, 2018, vol. 23, num. 3, p. E536 |
| URI: | http://hdl.handle.net/2445/122728 |
| Related resource: | https://doi.org/10.3390/molecules23030536 |
| ISSN: | 1420-3049 |
| Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) Articles publicats en revistes (Institut de Biomedicina (IBUB)) |
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|---|---|---|---|---|
| 679150.pdf | 2.8 MB | Adobe PDF | View/Open |
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