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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-10, Vol.8 (19), p.2737-2742
Hauptverfasser:	Regan, John, Bruno, Joseph, McGarry, Daniel, Poli, Gregory, Hanney, Barbara, Bower, Shelly, Travis, Jeffrey, Sweeney, Dennis, Miller, Bruce, Souness, John, Djuric, Stevan
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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