N-arylrolipram derivatives as potent and selective PDE4 inhibitors

被引：12

作者：

Bacher, E ^{[1
]}

Boer, C ^{[1
]}

Bray-French, K ^{[1
]}

Demnitz, FWJ ^{[1
]}

Keller, TH ^{[1
]}

Mazzoni, L ^{[1
]}

Müller, T ^{[1
]}

Walker, C ^{[1
]}

机构：

[1] Novartis Horsham Res Ctr, Resp Dis Therapeut Area, Horsham, W Sussex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(98)00583-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatization of rolipram led to the identification of 3-[4-(3-cyclopentyloxy-4-methoxyphenyl)-2-oxo-pynrolidin-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 pIC(50) 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.). (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3229 / 3234

页数：6

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