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2018-02-28

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cc-by (c) Leiva Martínez, Rosana et al., 2018
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/122728

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

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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.

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https://doi.org/10.3390/molecules23030536

Subject

Disseny de medicaments, Química farmacèutica, Enzims, Compostos policíclics

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Drug design, Pharmaceutical chemistry, Enzymes, Polycyclic compounds

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Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Biomedicina (IBUB))

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LEIVA MARTÍNEZ, Rosana, et al. Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 inhibitors. Molecules. 2018. Vol. 23, num. 3, pags. E536. ISSN 1420-3049. [consulted: 10 of October of 2026]. Available at: https://hdl.handle.net/2445/122728

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