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

The design and profile of a series of adamantyl-containing long acting beta sub(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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-02, Vol.18 (4), p.1280-1283
Main Authors: Brown, Alan D, Bunnage, Mark E, Glossop, Paul A, James, Kim, Jones, Rhys, Lane, Charlotte AL, Lewthwaite, Russell A, Mantell, Simon, Perros-Huguet, Christelle, Price, David A, Trevethick, Mike, Webster, Rob
Format: Article
Language:English
Online Access:Get full text
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Summary:The design and profile of a series of adamantyl-containing long acting beta sub(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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmcl.2008.01.034