Literature DB >> 16899366

Synthesis and biological evaluation of heterocycle containing adamantane 11beta-HSD1 inhibitors.

Vince S C Yeh1, Jyoti R Patel, Hong Yong, Ravi Kurukulasuriya, Steven Fung, Katina Monzon, William Chiou, Jiahong Wang, Deanne Stolarik, Hovis Imade, David Beno, Michael Brune, Peer Jacobson, Hing Sham, J T Link.   

Abstract

A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.

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Year:  2006        PMID: 16899366     DOI: 10.1016/j.bmcl.2006.07.055

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


  4 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.  In-silico identification of the binding mode of synthesized adamantyl derivatives inside cholinesterase enzymes.

Authors:  Amal Al-Aboudi; Raed A Al-Qawasmeh; Alaa Shahwan; Uzma Mahmood; Asaad Khalid; Zaheer Ul-Haq
Journal:  Acta Pharmacol Sin       Date:  2015-05-04       Impact factor: 6.150

Review 3.  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

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

  4 in total

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