PDE2 inhibition by the PI3 kinase inhibitor LY294002 and analogues

被引：24

作者：

Abbott, BM

Thompson, PE

机构：

[1] Monash Univ, Box Hill Hosp, Dept Med, Box Hill, Vic 3128, Australia

[2] Box Hill Hosp, Kinacia Pty Ltd, Box Hill, Vic 3128, Australia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 11期

基金：

澳大利亚研究理事会;

关键词：

phosphodiesterase; inhibitor; PDE2; LY294002; 2-morpholmochromone;

D O I：

10.1016/j.bmcl.2004.03.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthetic 2-morpholinochromones, including the known PI3-kinase inhibitor LY294002, have been evaluated in vitro as inhibitors of isolated human platelet phosphodiesterases. Inhibition of the cAMP-phosphodiesterases, PDE2 and PDE3 by LY294002 is reported for the first time. Preliminary screening across a range of 2-morpholinochromones has revealed structural features for optimised PDE2 inhibition. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2847 / 2851

页数：5

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