Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372265 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Spiro-carboxamides were identified as inhibitors of 11β-hydroxysteroid-dehydrogenase type 1 by high-throughput screening. Structure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC50 inhibitor (0.5 nM) on human 11β-HSD1 with a high binding efficiency index (BEI of 32.7) which was selective against human 11β-HSD2 (selectivity ratio > 200000).
Graphical abstractStructure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC50 inhibitor (0.5 nM) on human 11β-HSD1 with a high binding efficiency index (BEI of 32.7) which was selective against human 11β-HSD2 (selectivity ratio > 200000).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Chemistry
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Authors
Franck Lepifre, Serge Christmann-Franck, Didier Roche, Caroline Leriche, Denis Carniato, Christine Charon, Sophie Bozec, Liliane Doare, Fabien Schmidlin, Marc Lecomte, Eric Valeur,