Literature DB >> 18226900

The discovery of adamantyl-derived, inhaled, long acting beta(2)-adrenoreceptor agonists.

Alan D Brown1, Mark E Bunnage, Paul A Glossop, Kim James, Rhys Jones, Charlotte A L Lane, Russell A Lewthwaite, Simon Mantell, Christelle Perros-Huguet, David A Price, Mike Trevethick, Rob Webster.   

Abstract

The design and profile of a series of adamantyl-containing long acting beta(2)-adrenoreceptor agonists are described. An optimal pharmacokinetic profile of low oral bioavailability was combined with a strong pharmacology profile when assessed using a guinea pig trachea tissue model. A focus was then placed on developing a robust synthetic route to ensure rapid delivery of material for clinical trials.

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Year:  2008        PMID: 18226900     DOI: 10.1016/j.bmcl.2008.01.034

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


  3 in total

Review 1.  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

2.  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

3.  A Selective Pharmacophore Model for beta(2)-Adrenoceptor Agonists.

Authors:  Rui-Juan Xing; Jian Wang; Li Pan; Mao-Sheng Cheng
Journal:  Molecules       Date:  2009-11-06       Impact factor: 4.411

  3 in total

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