Document Detail


Third-generation long-acting β(2)-adrenoceptor agonists: medicinal chemistry strategies employed in the identification of once-daily inhaled β(2)-adrenoceptor agonists.
MedLine Citation:
PMID:  21942251     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Inhaled long-acting β(2)-adrenoceptor agonists (LABAs) are highly effective bronchodilators in the treatment of asthma and chronic obstructive pulmonary disease. There is significant interest in the development of third-generation compounds that improve upon the marketed twice-daily LABAs salmeterol and formoterol. A principal advantage sought from the next generation is duration of action that supports once-daily dosing, although improved efficacy, faster onset, and increased therapeutic index are also frequently cited as objectives. Recent publications detailing medicinal chemistry programs directed at the discovery of third-generation LABAs illustrate a wide variety of strategies that have been successfully employed towards these goals. Some recent scientific advances in the understanding of inhaled bronchodilators are discussed and the reported medicinal chemistry strategies are reviewed in the context of these advances.
Authors:
John R Jacobsen
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Future medicinal chemistry     Volume:  3     ISSN:  1756-8927     ISO Abbreviation:  Future Med Chem     Publication Date:  2011 Oct 
Date Detail:
Created Date:  2011-09-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101511162     Medline TA:  Future Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  1607-22     Citation Subset:  IM    
Affiliation:
Theravance, Inc., 901 Gateway Blvd, South San Francisco, CA 94080, USA. jjacobsen@theravance.com.
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