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ID: ALA1130674
Journal: Bioorg Med Chem Lett
Title: N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
Authors: Bacher E, Boer C, Bray-French K, Demnitz FW, Keller TH, Mazzoni L, Müller T, Walker C.
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.).
CiteXplore: 9873708