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

[Display omitted] The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11β-HSD1 inhibitors and the serendipitous discovery of β-keto sulfones as potent 11β-HSD1 inhibitors are described here. These two classes of compounds are not active against 11β-HSD2 and therefore may h...

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Published inBioorganic & medicinal chemistry letters Vol. 15; no. 11; pp. 2865 - 2869
Main Authors Xiang, Jason, Ipek, Manus, Suri, Vipin, Massefski, Walt, Pan, Ning, Ge, Ying, Tam, May, Xing, Yuzhe, Tobin, James F., Xu, Xin, Tam, Steve
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 02.06.2005
Elsevier
Subjects
11β-HSD1
Biological and medical sciences
General and cellular metabolism. Vitamins
Inhibitor
Medical sciences
Pharmacology. Drug treatments
Sulfonamidooxazole
β-Keto sulfone
Inhibitor
Sulfonamidooxazole
11β-HSD1
β-Keto sulfone
Type 2 diabetes
Five membered ring
Sulfonamide
Sulfone
Enzyme
Benzene derivatives
Enzyme inhibitor
Selectivity
Oxosulfone
Metabolic disorder
Structure activity relation
Biphenyl derivatives
11β-Hydroxysteroid dehydrogenase
Oxidoreductases
Fluorine Organic compounds
Chemical synthesis
Oxazole derivatives
Oxygen nitrogen heterocycle
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Summary:[Display omitted] The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11β-HSD1 inhibitors and the serendipitous discovery of β-keto sulfones as potent 11β-HSD1 inhibitors are described here. These two classes of compounds are not active against 11β-HSD2 and therefore may have significant therapeutic potential for metabolic syndrome, type 2 diabetes and related metabolic dysfunctions.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.03.093