| Literature DB >> 19395260 |
Didier Roche1, Denis Carniato, Caroline Leriche, Franck Lepifre, Serge Christmann-Franck, Ulrich Graedler, Christine Charon, Sophie Bozec, Liliane Doare, Fabien Schmidlin, Marc Lecomte, Eric Valeur.
Abstract
Benzylamides of pentanedioic acid were identified as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) by high-throughput screening. Optimisation to 2-adamantyl amides yielded inhibitors with single digit nanomolar IC(50)s on the 11beta-HSD1 human isoform. The hydroxy adamantyl amide lead compound was selective against 11beta-hydroxysteroid dehydrogenase type 2 (selectivity ratio >1000) and displayed good inhibition of 11beta-HSD1 (IC(50)<0.1microM) in a cellular model (3T3L1 adipocytes).Entities:
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Year: 2009 PMID： 19395260 DOI： 10.1016/j.bmcl.2009.03.140
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823