AWD 12-281 - Antiasthmatic/antiinflammatory - Phosphodiesterase 4 inhibitor

被引:6
作者
Kuss, H
Hofgen, N
Egerland, U
Heer, S
Marx, D
Szelenyi, I
Schupke, H
Gasparic, A
Olbrich, M
Hempel, R
Hartenhauer, H
Krone, D
Berthold, K
Kronbach, T
Runfeldt, C
机构
[1] Arzneimittelwerk Dresden GmbH, D-01445 Radebeul, Germany
[2] ASTA Medica AG, D-60001 Frankfurt, Germany
关键词
D O I
10.1358/dof.2002.027.02.651710
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Airway diseases such as bronchial asthma and chronic obstructive pulmonary disease (COPD) are chronic inflammatory diseases whose prevalence is increasing. Current research concerned with developing effective treatments for these conditions have focused on the search for alternatives to the standard corticosteroid antiinflammatory therapy. Selective phosphodiesterase 4 (PDE4) inhibitors have received a considerable amount of attention due to their ability to suppress the functions of several cell types involved in allergic and inflammatory disorders. The selective PDE4 inhibitor AWD 12-281 is the result of a pharmacophore-based synthesis program wherein the optimization process was supported by ligand-based drug design methods. AWD 12-281 was selected for further development for its high affinity and selectivity for the human PDE4 isoenzyme and due to its potent activity and excellent tolerability in models of allergic rhinitis, asthma and COPD, especially after topical treatment.
引用
收藏
页码:111 / 116
页数:6
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