Literature DB >> 16039856

Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Steven Olson1, Susan D Aster, Kai Brown, Linda Carbin, Donald W Graham, Anne Hermanowski-Vosatka, Cheryl B LeGrand, Steven S Mundt, Michael A Robbins, James M Schaeffer, Llnon H Slossberg, Michael J Szymonifka, Rolf Thieringer, Samuel D Wright, James M Balkovec.   

Abstract

Adamantyl triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active both in in vitro and in in vivo pharmacodynamic models. The synthesis and structure-activity relationships of these inhibitors are presented.

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Year:  2005        PMID: 16039856     DOI: 10.1016/j.bmcl.2005.06.040

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


  8 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

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.  Visceral adipose tissue: emerging role of gluco- and mineralocorticoid hormones in the setting of cardiometabolic alterations.

Authors:  Marco Boscaro; Gilberta Giacchetti; Vanessa Ronconi
Journal:  Ann N Y Acad Sci       Date:  2012-07-17       Impact factor: 5.691

4.  Antimicrobial and hypoglycemic activities of novel N-Mannich bases derived from 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thiones.

Authors:  Ebtehal S Al-Abdullah; Hanaa M Al-Tuwaijri; Hanan M Hassan; Mogedda E Haiba; Elsayed E Habib; Ali A El-Emam
Journal:  Int J Mol Sci       Date:  2014-12-11       Impact factor: 5.923

5.  Adamantane-Isothiourea Hybrid Derivatives: Synthesis, Characterization, In Vitro Antimicrobial, and In Vivo Hypoglycemic Activities.

Authors:  Lamya H Al-Wahaibi; Hanan M Hassan; Amal M Abo-Kamar; Hazem A Ghabbour; Ali A El-Emam
Journal:  Molecules       Date:  2017-04-29       Impact factor: 4.411

6.  Crystal structure, Hirshfeld surface analysis and DFT studies of 5-(adamantan-1-yl)-3-[(4-chlorobenzyl)sulfanyl]-4-methyl-4H-1,2,4-triazole, a potential 11β-HSD1 inhibitor.

Authors:  Lamya H Al-Wahaibi; Jacques Joubert; Olivier Blacque; Nora H Al-Shaalan; Ali A El-Emam
Journal:  Sci Rep       Date:  2019-12-24       Impact factor: 4.379

7.  Synthesis, Characterization and Biological Evaluation of Metal Adamantyl 2-Pyridylhydrazone Complexes.

Authors:  Ihsan A Shehadi; Fatima-Azzahra Delmani; Areej M Jaber; Hana Hammad; Murad A AlDamen; Raed A Al-Qawasmeh; Monther A Khanfar
Journal:  Molecules       Date:  2020-05-29       Impact factor: 4.411

8.  Synthesis, Characterization, Crystal Structure, and DFT Study of a New Square Planar Cu(II) Complex Containing Bulky Adamantane Ligand.

Authors:  Monther A Khanfar; Areej M Jaber; Murad A AlDamen; Raed A Al-Qawasmeh
Journal:  Molecules       Date:  2018-03-20       Impact factor: 4.411

  8 in total

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