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.
Regan
J
J
Rhône-Poulenc Rorer, Collegeville, PA 19426, USA.
Bruno
J
J
McGarry
D
D
Poli
G
G
Hanney
B
B
Bower
S
S
Travis
J
J
Sweeney
D
D
Miller
B
B
Souness
J
J
Djuric
S
S
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D007700:Kinetics; D051379:Mice; D010084:Oxidation-Reduction; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D012995:Solubility; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4