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ID: ALA1139567

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Authors: Xiang J, Ipek M, Suri V, Massefski W, Pan N, Ge Y, Tam M, Xing Y, Tobin JF, Xu X, Tam S.

Abstract: The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11beta-HSD1 inhibitors and the serendipitous discovery of beta-keto sulfones as potent 11beta-HSD1 inhibitors are described here. These two classes of compounds are not active against 11beta-HSD2 and therefore may have significant therapeutic potential for metabolic syndrome, type 2 diabetes and related metabolic dysfunctions.

CiteXplore: 15911270

DOI: 10.1016/j.bmcl.2005.03.093