Literature DB >> 21652207

Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.

Michael J Stocks1, Lilian Alcaraz, Andrew Bailey, Roger Bonnert, Elaine Cadogan, Jadeen Christie, Stephen Connolly, Anthony Cook, Adrian Fisher, Alice Flaherty, Stephen Hill, Alexander Humphries, Anthony Ingall, Stephen Jordan, Mandy Lawson, Alex Mullen, David Nicholls, Stuart Paine, Garry Pairaudeau, Stephen St-Gallay, Alan Young.   

Abstract

The design and synthesis of a new series of high efficacy β(2)-agonists devoid of the key benzylic alcohol present in previously described highly efficacious β(2)-agonists is reported. A hypothesis for the unprecedented level of efficacy is proposed based on considerations of β(2)-adrenoceptor crystal structure, other biophysical data and modeling studies.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21652207     DOI: 10.1016/j.bmcl.2011.04.135

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


  1 in total

1.  Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.

Authors:  Michael J Stocks; Lilian Alcaraz; Andrew Bailey; Roger Bonnert; Elaine Cadogan; Jadeen Christie; John Dixon; Stephen Connolly; Anthony Cook; Adrian Fisher; Alice Flaherty; Alexander Humphries; Anthony Ingall; Stephen Jordan; Mandy Lawson; Alex Mullen; David Nicholls; Stuart Paine; Garry Pairaudeau; Alan Young
Journal:  ACS Med Chem Lett       Date:  2014-02-08       Impact factor: 4.345

  1 in total

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