Details

Autor(en) / Beteiligte

• Mantell, Simon J
• Stephenson, Peter T
• Monaghan, Sandra M
• Maw, Graham N
• Trevethick, Michael A
• Yeadon, Michael
• Keir, Ruth F
• Walker, Don K
• Jones, Rhys M
• Selby, Matthew D
• Batchelor, David V
• Rozze, Stuart
• Chavaroche, Helene
• Hobson, Tim J
• Dodd, Peter G
• Lemaitre, Arnaud
• Wright, Karen N
• Stuart, Emilio F

Titel

Inhaled adenosine A sub(2A) receptor agonists for the treatment of chronic obstructive pulmonary disease

Ist Teil von

• Bioorganic & medicinal chemistry, 2008-02, Vol.18 (4), p.1284-1287

Erscheinungsjahr

2008

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• COPD is a major cause of mortality in the western world. A sub(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A sub(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 sub(2A) agonists described. A sevenfold improvement in potency and 150-fold reduction in side-effect liability over the lead compound CGS-21680, were obtained.