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Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Wed, 01/02/2013 - 10:11am — ccarey
| Title | Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
| Publication Type | Journal Article |
| Year of Publication | 2005 |
| Authors | Xiang, J, Ipek, M, Suri, V, Massefski, W, Pan, N, Ge, Y, Tam, M, Xing, Y, Tobin, JF, Xu, X, Tam, S |
| Journal | Bioorg Med Chem Lett |
| Volume | 15 |
| Issue | 11 |
| Pagination | 2865-9 |
| Date Published | 2005 Jun 2 |
| ISSN | 0960-894X |
| Keywords | 11-beta-Hydroxysteroid Dehydrogenase Type 1, Enzyme Inhibitors, Oxazoles, Structure-Activity Relationship, Sulfones |
| 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. |
| DOI | 10.1016/j.bmcl.2005.03.093 |
| Custom 1 | |
| Alternate Journal | Bioorg. Med. Chem. Lett. |
| PubMed ID | 15911270 |
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