期刊
ACS OMEGA
卷 3, 期 8, 页码 8843-8853出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.8b01214
关键词
-
资金
- European Union (European Regional Development Fund-ERDF)
- Greek national funds through the Operational Program Competitiveness and Entrepreneurship of the National Strategic Reference Framework (NSRF)-Research Funding Program: Phospholipases A2 inhibitors: Developing a drug pipeline for the treatment of inflam
- NIH [GM20501-42]
- National Scholarship Foundation (IKY)
Cytosolic phospholipase A(2) (GrvA cPLA(2)) has attracted great interest as a medicinal target because it initiates the eicosanoid cascade and is involved in a number of inflammatory diseases. As consequence, the development of potent synthetic inhibitors is of great importance We have developed highly potent 2-oxoester inhibitors of GIVA cPLA(2) presenting X-I (50) values between 0 000019 and 0 000066 We demonstrate that the 2-oxoester functionality is essential for in vitro inhibitory activity, making these inhibitors useful research reagents. However, their high reactivity results in rapid degradation of the inhibitors in human plasma, limiting their pharmaceutical utility without further modification.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据