2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors

J Regan; J Bruno; D McGarry; G Poli; B Hanney; S Bower; J Travis; D Sweeney; B Miller; J Souness; S Djuric

doi:10.1016/s0960-894x(98)00497-1

2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2737-42. doi: 10.1016/s0960-894x(98)00497-1.

Authors

J Regan¹, J Bruno, D McGarry, G Poli, B Hanney, S Bower, J Travis, D Sweeney, B Miller, J Souness, S Djuric

Affiliation

¹ Rhône-Poulenc Rorer, Collegeville, PA 19426, USA.

PMID: 9873613
DOI: 10.1016/s0960-894x(98)00497-1

Abstract

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.

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
Animals
Benzimidazoles / chemical synthesis*
Benzimidazoles / metabolism
Benzimidazoles / pharmacology*
Cyclic Nucleotide Phosphodiesterases, Type 4
Kinetics
Mice
Oxidation-Reduction
Phosphodiesterase Inhibitors / chemical synthesis*
Phosphodiesterase Inhibitors / metabolism
Phosphodiesterase Inhibitors / pharmacology*
Rats
Solubility
Structure-Activity Relationship

Substances

Benzimidazoles
Phosphodiesterase Inhibitors
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 4