| Literature DB >> 18243699 |
Simon J Mantell1, Peter T Stephenson, Sandra M Monaghan, Graham N Maw, Michael A Trevethick, Michael Yeadon, Ruth F Keir, Don K Walker, Rhys M Jones, Matthew D Selby, David V Batchelor, Stuart Rozze, Helene Chavaroche, Tim J Hobson, Peter G Dodd, Arnaud Lemaitre, Karen N Wright, Emilio F Stuart.
Abstract
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be therapeutically useful. A strategy of minimizing side-effect liability by maximizing systemic clearance was followed and pharmacological and pharmacokinetic SAR of a series of inhaled A(2A) agonists described. A sevenfold improvement in potency and 150-fold reduction in side-effect liability over the lead compound CGS-21680, were obtained.Entities:
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Year: 2008 PMID： 18243699 DOI： 10.1016/j.bmcl.2008.01.033
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823