Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373028 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
COPD is a major cause of mortality in the western world. A2A agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A2A 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 A2A agonists described. A sevenfold improvement in potency and 150-fold reduction in side-effect liability over the lead compound CGS-21680, were obtained.
Graphical abstractThe pharmacological and pharmacokinetic SAR of a series of inhaled A2A agonists for the treatment of chronic obstructive pulmonary disease is described.Figure optionsDownload full-size imageDownload as PowerPoint slide