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N-arylrolipram derivatives as potent and selective PDE4 inhibitors
E Bacher1, C Boer, K Bray-French
1Respiratory Disease Therapeutic Area, Novartis Horsham Research Center, West Sussex, UK.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
Derivatization of rolipram led to the identification of 3-[4-(3-cyclopentyloxy-4-methoxyphenyl)-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.).