Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363751 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Substituted 8-arylquinoline analogs bearing alkyl-linked side chain were identified as potent inhibitors of type 4 phophodiesterase. These compounds address the potential liabilities of the clinical candidate L-454560. The pharmacokinetic profile of the best analogs and the in vivo efficacy in an ovalbumin-induced bronchoconstriction assay in conscious guinea pigs are reported.
Graphical abstractPotent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs bearing alkyl-linked side chain were identified as potent inhibitors based on the SAR described herein.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Patrick Lacombe, Nathalie Chauret, David Claveau, Stephen Day, Denis Deschênes, Daniel Dubé, Michel Gallant, Yves Girard, Zheng Huang, France Laliberté, Jean-Francois Lévesque, Susana Liu, Dwight Macdonald, Joseph A. Mancini, Paul Masson,