کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1373028 | 981888 | 2008 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Inhaled adenosine A2A receptor agonists for the treatment of chronic obstructive pulmonary disease Inhaled adenosine A2A receptor agonists for the treatment of chronic obstructive pulmonary disease](/preview/png/1373028.png)
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.
The pharmacological and pharmacokinetic SAR of a series of inhaled A2A agonists for the treatment of chronic obstructive pulmonary disease is described.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 4, 15 February 2008, Pages 1284–1287