| Autor: |
Mantell SJ; Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Kent CT13 9NJ, United Kingdom., Stephenson PT, Monaghan SM, Maw GN, Trevethick MA, Yeadon M, Keir RF, Walker DK, Jones RM, Selby MD, Batchelor DV, Rozze S, Chavaroche H, Hobson TJ, Dodd PG, Lemaitre A, Wright KN, Stuart EF |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 15; Vol. 18 (4), pp. 1284-7. Date of Electronic Publication: 2008 Jan 12. |
| DOI: |
10.1016/j.bmcl.2008.01.033 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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