2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors

A new family of PDE4 inhibitors based on a benzimidazole framework is described. Several of these compounds are orally bioavailable and show efficacy in in vivo models of inflammatory disease. A new family of PDE4 inhibitors based on a benzimidazole framework is described. Several of these compounds...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2737-2742
Main Authors: Regan, John, Bruno, Joseph, McGarry, Daniel, Poli, Gregory, Hanney, Barbara, Bower, Shelly, Travis, Jeffrey, Sweeney, Dennis, Miller, Bruce, Souness, John, Djuric, Stevan
Format: Article
Language:English
Subjects:
3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors
Animals
Benzimidazoles - chemical synthesis
Benzimidazoles - metabolism
Benzimidazoles - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclic Nucleotide Phosphodiesterases, Type 4
Kinetics
Medical sciences
Mice
Oxidation-Reduction
Pharmacology. Drug treatments
Phosphodiesterase Inhibitors - chemical synthesis
Phosphodiesterase Inhibitors - metabolism
Phosphodiesterase Inhibitors - pharmacology
Rats
Solubility
Structure-Activity Relationship
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Summary:A new family of PDE4 inhibitors based on a benzimidazole framework is described. Several of these compounds are orally bioavailable and show efficacy in in vivo models of inflammatory disease. A new family of PDE4 inhibitors based on a benzimidazole framework is described. Several of these compounds are orally bioavailable and show efficacy in in vivo models of inflammatory disease.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00497-1