Literature DB >> 17000111

Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.

Steven Richards1, Bryan Sorensen, Hwan-Soo Jae, Marty Winn, Yixian Chen, Jiahong Wang, Steven Fung, Katina Monzon, Ernst U Frevert, Peer Jacobson, Hing Sham, J T Link.   

Abstract

High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.

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Year:  2006        PMID: 17000111     DOI: 10.1016/j.bmcl.2006.09.035

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Stereocontrolled synthesis and pharmacological evaluation of cis-2,6-diphenethyl-1-azabicyclo[2.2.2]octanes as lobelane analogues.

Authors:  Guangrong Zheng; Linda P Dwoskin; Agripina G Deaciuc; Peter A Crooks
Journal:  J Org Chem       Date:  2009-08-21       Impact factor: 4.354

2.  Exploring N-acyl-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-enes as 11β-HSD1 Inhibitors.

Authors:  Rosana Leiva; Andrew McBride; Margaret Binnie; Scott P Webster; Santiago Vázquez
Journal:  Molecules       Date:  2018-02-28       Impact factor: 4.411

  2 in total

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