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Extensive structural modifications to the 18beta-glycyrrhetinic acid template are described and their effects on the SAR of the 11beta-hydroxysteroid dehydrogenase isozymes type 1 and 2 from the rat are investigated. Isoform selective inhibitors have been discovered and compound 7 N-(2-hydroxyethyl)-3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic acid amide is highlighted as a very potent selective inhibitor of 11beta-hydroxysteroid dehydrogenase 2 with an IC(50) = 4pM.

Original publication

DOI

10.1016/j.bmc.2004.06.008

Type

Journal article

Journal

Bioorg Med Chem

Publication Date

15/08/2004

Volume

12

Pages

4439 - 4457

Keywords

11-beta-Hydroxysteroid Dehydrogenase Type 2, Animals, Enzyme Inhibitors, Glycyrrhetinic Acid, Oleanolic Acid, Rats