Literature DB >> 17490884

beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.

Jason Xiang1, Manus Ipek, Vipin Suri, May Tam, Yuzhe Xing, Nelson Huang, Yanling Zhang, James Tobin, Tarek S Mansour, John McKew.   

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.

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Year:  2007        PMID： 17490884     DOI： 10.1016/j.bmc.2007.04.035

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  6 in total

1.  Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.

Authors:  Scott P Webster; Margaret Binnie; Kirsty M M McConnell; Karen Sooy; Peter Ward; Michael F Greaney; Andy Vinter; T David Pallin; Hazel J Dyke; Matthew I A Gill; Ines Warner; Jonathan R Seckl; Brian R Walker
Journal:  Bioorg Med Chem Lett       Date:  2010-04-18       Impact factor: 2.823

2.  Aerobic oxidation in nanomicelles of aryl alkynes, in water at room temperature.

Authors:  Sachin Handa; James C Fennewald; Bruce H Lipshutz
Journal:  Angew Chem Int Ed Engl       Date:  2014-02-24       Impact factor: 15.336

3.  Studies on the chemistry and reactivity of alpha-substituted ketones in isonitrile-based multicomponent reactions.

Authors:  Lijun Fan; Ashley M Adams; Jason G Polisar; Bruce Ganem
Journal:  J Org Chem       Date:  2008-12-19       Impact factor: 4.354

4.  Pyrimidine Nucleosides with a Reactive (β-Chlorovinyl)sulfone or (β-Keto)sulfone Group at the C5 Position, Their Reactions with Nucleophiles and Electrophiles, and Their Polymerase-Catalyzed Incorporation into DNA.

Authors:  Sazzad H Suzol; A Hasan Howlader; Zhiwei Wen; Yaou Ren; Eduardo E Laverde; Carol Garcia; Yuan Liu; Stanislaw F Wnuk
Journal:  ACS Omega       Date:  2018-04-16

5.  Non-invasive in vivo assessment of 11β-hydroxysteroid dehydrogenase type 1 activity by 19F-Magnetic Resonance Spectroscopy.

Authors:  Brian R Walker; Ruth Andrew; Gregorio Naredo-Gonzalez; Rita Upreti; Maurits A Jansen; Scott Semple; Oliver B Sutcliffe; Ian Marshall
Journal:  Sci Rep       Date:  2022-09-29       Impact factor: 4.996

6.  Manganese(III) acetate-mediated oxidative cyclization of a-methylstyrene and trans-stilbene with b-ketosulfones.

Authors:  Ahlem Bouhlel; Christophe Curti; Clémence Tabelé; Patrice Vanelle
Journal:  Molecules       Date:  2013-04-11       Impact factor: 4.411
  6 in total

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