Literature DB >> 17350260

Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.

Scott P Webster1, Peter Ward, Margaret Binnie, Eilidh Craigie, Kirsty M M McConnell, Karen Sooy, Andy Vinter, Jonathan R Seckl, Brian R Walker.   

Abstract

A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

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Year:  2007        PMID： 17350260     DOI： 10.1016/j.bmcl.2007.02.057

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


  14 in total

1.  High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

Authors:  Subramaniam Ananthan; Ellen R Faaleolea; Robert C Goldman; Judith V Hobrath; Cecil D Kwong; Barbara E Laughon; Joseph A Maddry; Alka Mehta; Lynn Rasmussen; Robert C Reynolds; John A Secrist; Nice Shindo; Dustin N Showe; Melinda I Sosa; William J Suling; E Lucile White
Journal:  Tuberculosis (Edinb)       Date:  2009-09-15       Impact factor: 3.131

Review 2.  The lipophilic bullet hits the targets: medicinal chemistry of adamantane derivatives.

Authors:  Lukas Wanka; Khalid Iqbal; Peter R Schreiner
Journal:  Chem Rev       Date:  2013-02-25       Impact factor: 60.622

3.  11beta-hydroxysteroid dehydrogenase type 1 expression is increased in the aged mouse hippocampus and parietal cortex and causes memory impairments.

Authors:  Megan C Holmes; Roderick N Carter; June Noble; Shruti Chitnis; Amy Dutia; Janice M Paterson; John J Mullins; Jonathan R Seckl; Joyce L W Yau
Journal:  J Neurosci       Date:  2010-05-19       Impact factor: 6.167

4.  Continuous inhibition of 11β-hydroxysteroid dehydrogenase type I in adipose tissue leads to tachyphylaxis in humans and rats but not in mice.

Authors:  P Morentin Gutierrez; A Gyte; J deSchoolmeester; P Ceuppens; J Swales; C Stacey; J W Eriksson; M Sjöstrand; C Nilsson; B Leighton
Journal:  Br J Pharmacol       Date:  2015-10-08       Impact factor: 8.739

5.  Synthesis and characterization of 2-substituted bornane pharmacophores for novel cannabinergic ligands.

Authors:  Richard I Duclos; Dai Lu; Jianxin Guo; Alexandros Makriyannis
Journal:  Tetrahedron Lett       Date:  2008-09-22       Impact factor: 2.415

6.  Partial deficiency or short-term inhibition of 11beta-hydroxysteroid dehydrogenase type 1 improves cognitive function in aging mice.

Authors:  Karen Sooy; Scott P Webster; June Noble; Margaret Binnie; Brian R Walker; Jonathan R Seckl; Joyce L W Yau
Journal:  J Neurosci       Date:  2010-10-13       Impact factor: 6.167

7.  11β-Hydroxysteroid dehydrogenase type 1 contributes to the balance between 7-keto- and 7-hydroxy-oxysterols in vivo.

Authors:  Tijana Mitić; Steven Shave; Nina Semjonous; Iain McNae; Diego F Cobice; Gareth G Lavery; Scott P Webster; Patrick W F Hadoke; Brian R Walker; Ruth Andrew
Journal:  Biochem Pharmacol       Date:  2013-02-13       Impact factor: 5.858

8.  Local amplification of glucocorticoids in the aging brain and impaired spatial memory.

Authors:  Joyce L W Yau; Jonathan R Seckl
Journal:  Front Aging Neurosci       Date:  2012-08-29       Impact factor: 5.750

9.  Recycling between cortisol and cortisone in human splanchnic, subcutaneous adipose, and skeletal muscle tissues in vivo.

Authors:  Katherine A Hughes; Konstantinos N Manolopoulos; Javaid Iqbal; Nicholas L Cruden; Roland H Stimson; Rebecca M Reynolds; David E Newby; Ruth Andrew; Fredrik Karpe; Brian R Walker
Journal:  Diabetes       Date:  2012-04-17       Impact factor: 9.461

10.  Identification of important chemical features of 11β-hydroxysteroid dehydrogenase type1 inhibitors: application of ligand based virtual screening and density functional theory.

Authors:  Sugunadevi Sakkiah; Chandrasekaran Meganathan; Young-Sik Sohn; Sundaraganesan Namadevan; Keun Woo Lee
Journal:  Int J Mol Sci       Date:  2012-04-23       Impact factor: 6.208
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