Literature DB >> 21723724

Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists.

Stephen Connolly1, Lilian Alcaraz, Andrew Bailey, Elaine Cadogan, Jadeen Christie, Anthony R Cook, Adrian J Fisher, Stephen Hill, Alexander Humphries, Anthony H Ingall, Zoe Kane, Stuart Paine, Garry Pairaudeau, Michael J Stocks, Alan Young.   

Abstract

Starting with the molecular scaffold of the DA(2)/β(2) dual agonist sibenadet (Viozan™), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its pharmacokinetics. Through this process a novel, high potency, full β(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered.
Copyright © 2011. Published by Elsevier Ltd.

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Year:  2011        PMID: 21723724     DOI: 10.1016/j.bmcl.2011.05.097

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


  3 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

2.  Design, Synthesis, and Evaluation of Lung-Retentive Prodrugs for Extending the Lung Tissue Retention of Inhaled Drugs.

Authors:  Jack Ayre; Joanna M Redmond; Giovanni Vitulli; Laura Tomlinson; Richard Weaver; Eleonora Comeo; Cynthia Bosquillon; Michael J Stocks
Journal:  J Med Chem       Date:  2022-07-07       Impact factor: 8.039

Review 3.  Multitargeting nature of muscarinic orthosteric agonists and antagonists.

Authors:  Jaromir Myslivecek
Journal:  Front Physiol       Date:  2022-09-06       Impact factor: 4.755

  3 in total

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