N-arylrolipram derivatives as potent and selective PDE4 inhibitors

Article abstract of DOI:10.1016/S0960-894X(98)00583-6

Derivatization of rolipram led to the identification of 3-[4-(3- cyclopentyloxy-4-methoxypbenyl)-2-oxo-pyrrolidin-1-yl]-5-(3- methoxybenzyloxy)-benzoic acid N',N'-dimethylhydrazide (4), a potent and selective inhibitor of PDE4, which inhibits the activation of human leukocytes with pIC₅₀ values in the range of 7.3 - 7.8, and blocks antigen induced eosinophilia in Brown Norway rats at a dose of 1 mg/kg (i.t.).