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Bioorg Med Chem Lett. 1998 Nov 17;8(22):3229-34.

N-arylrolipram derivatives as potent and selective PDE4 inhibitors.

Author information

1
Respiratory Disease Therapeutic Area, Novartis Horsham Research Center, West Sussex, UK.

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.).

PMID:
9873708
DOI:
10.1016/s0960-894x(98)00583-6
[Indexed for MEDLINE]

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