220284-70-8Relevant articles and documents
N-arylrolipram derivatives as potent and selective PDE4 inhibitors
Bacher, Edmond,Boer, Christiene,Bray-French, Katharine,Demnitz, F. W. Joachim,Keller, Thomas H.,Mazzoni, Lazzaro,Mueller, Thomas,Walker, Christoph
, p. 3229 - 3234 (1998)
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.).
Synthesis of N-arylrolipram derivatives - Potent and selective phosphodiesterase-IV inhibitors - by copper catalyzed lactam-aryl halide coupling
Aebischcr, Esther,Bacher, Edmond,Joachim Demnitz,Keller, Thomas H.,Kurzmeyer, Miriam,Ortiz, Marta L.,Pombo-Villar, Esteban,Weber, Hans-Peter
, p. 2225 - 2229 (2007/10/03)
The copper catalysed coupling of rolipram (1) with a wide variety of aryl halides (2) affords N-arylrolipram derivatives (3), potent and selective phosphodiesterase type-IV inhibitors.