Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I |
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Authors: | Xiang Jason Ipek Manus Suri Vipin Massefski Walt Pan Ning Ge Ying Tam May Xing Yuzhe Tobin James F Xu Xin Tam Steve |
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Affiliation: | Chemical and Screening Sciences, Wyeth Research, MA 02140, USA. jxiang@wyeth.com |
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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. |
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