title: beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
abstract: The design, synthesis, and biological evaluation of beta-keto sulfones as 11beta-HSD1 inhibitors and the mechanism of inhibition are described here. This class of compounds is not active against 11beta-HSD2 and therefore may have therapeutic potential for metabolic syndrome and type 2 diabetes.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, MA 02140, USA. jxiang@wyeth.com
authors.forename: Jason
authors.initials: J
authors.lastname: Xiang
authors.forename: Manus
authors.initials: M
authors.lastname: Ipek
authors.forename: Vipin
authors.initials: V
authors.lastname: Suri
authors.forename: May
authors.initials: M
authors.lastname: Tam
authors.forename: Yuzhe
authors.initials: Y
authors.lastname: Xing
authors.forename: Nelson
authors.initials: N
authors.lastname: Huang
authors.forename: Yanling
authors.initials: Y
authors.lastname: Zhang
authors.forename: James
authors.initials: J
authors.lastname: Tobin
authors.forename: Tarek S
authors.initials: TS
authors.lastname: Mansour
authors.forename: John
authors.initials: J
authors.lastname: McKew
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000478:Alkylation; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004563:Electrochemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007659:Ketones / Q000138:chemical synthesis* / Q000494:pharmacology*; D012997:Solvents; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007659:Ketones; D012997:Solvents; D013450:Sulfones; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1