Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors

被引：38

作者：

Donnell, Andrew F. ^{[1
]}

Dollings, Paul J. ^{[1
]}

Butera, John A. ^{[1
]}

Dietrich, Arlene J. ^{[1
]}

Lipinski, Kerri K. ^{[2
]}

Ghavami, Afshin ^{[2
]}

Hirst, Warren D. ^{[2
]}

机构：

[1] Pfizer Global Res & Dev, Worldwide Med Chem, Princeton, NJ 08543 USA

[2] Pfizer Global Res & Dev, Neurosci Res Unit, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期

关键词：

Selective phosphodiesterase inhibitors; Pyridazino[4,5-b]indolizines; Hit-to-lead; PHOSPHODIESTERASE INHIBITORS; ROLIPRAM; ENHANCEMENT; MEMORY; TARGET;

D O I：

10.1016/j.bmcl.2010.02.044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Substituted pyridazino[4,5-b]indolizines were identified as potent and selective PDE4B inhibitors. We describe the structure-activity relationships generated around an HTS hit that led to a series of compounds with low nanomolar affinity for PDE4B and high selectivity over the PDE4D subtype. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2163 / 2167

页数：5

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