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Start Over Author "Yuzhe Xing" Journal bioorganic & medicinal chemistry letters
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1. Synthesis and biological evaluation of sulfonamidooxazoles and β-keto sulfones: selective inhibitors of 11β-hydroxysteroid dehydrogenase type I

Author

Yuzhe Xing, Walt Massefski, Manus Ipek, Ning Pan, Tam Steve Yik-Kai, Vipin Suri, Xin Xu, May Tam, James Tobin, Ying Ge, and Jason Shaoyun Xiang

Subjects
Clinical Biochemistry, Pharmaceutical Science, Type 2 diabetes, Biochemistry, Chemical synthesis, Sulfone, Structure-Activity Relationship, chemistry.chemical_compound, 11-beta-Hydroxysteroid Dehydrogenase Type 1, Drug Discovery, medicine, Structure–activity relationship, Sulfones, Enzyme Inhibitors, Oxazoles, Molecular Biology, chemistry.chemical_classification, biology, Organic Chemistry, Sulfonamide (medicine), Metabolic disorder, medicine.disease, Enzyme, chemistry, Enzyme inhibitor, biology.protein, Molecular Medicine, hormones, hormone substitutes, and hormone antagonists, medicine.drug
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.

Published
2005

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