8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma

A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4). A series of bicyclic heteroaryl ring syste...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-06, Vol.12 (12), p.1613-1615
Main Authors: Buckley, George M., Cooper, Nicola, Dyke, Hazel J., Galleway, Fiona P., Gowers, Lewis, Haughan, Alan F., Kendall, Hannah J., Lowe, Christopher, Maxey, Robert, Montana, John G., Naylor, Robert, Oxford, Janet, Peake, Joanna C., Picken, C.Louise, Runcie, Karen A., Sabin, Verity, Sharpe, Andrew, Warneck, Julie B.H.
Format: Article
Language:English
Subjects:
3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors
Amides - pharmacology
Amides - therapeutic use
Anti-Asthmatic Agents - pharmacology
Anti-Asthmatic Agents - therapeutic use
Asthma - drug therapy
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclic Nucleotide Phosphodiesterases, Type 4
Humans
Medical sciences
Pharmacology. Drug treatments
Phosphodiesterase Inhibitors - pharmacology
Phosphodiesterase Inhibitors - therapeutic use
Respiratory system
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Summary:A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4). A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase 4.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00223-8