N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
作者信息
Bacher E, Boer C, Bray-French K, Demnitz F W, Keller T H, Mazzoni L, Müller T, Walker C
机构信息
Respiratory Disease Therapeutic Area, Novartis Horsham Research Center, West Sussex, UK.
出版信息
Bioorg Med Chem Lett. 1998 Nov 17;8(22):3229-34. doi: 10.1016/s0960-894x(98)00583-6.
PMID:9873708
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.).
摘要
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