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题名: Structure-based design and synthesis of novel type quinoline as secretory PLA(2) inhibitors
作者: Liu, Y;  Feng, YB;  Gao, Y;  Wang, RX;  Lai, LH
关键词: design ;  synthesis ;  quinoline ;  PLA(2) inhibitor ;  bioactivity
刊名: ACTA CHIMICA SINICA
发表日期: 2001
卷: 59, 期:10, 页:1751-1755
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Physical Sciences
类目[WOS]: Chemistry, Multidisciplinary
研究领域[WOS]: Chemistry
英文摘要: Phospholipase A2 (PLA(2)) plays an important role in the pathology of a number of human diseases and is an attract target for medicinal chemistry research. Therefore, the development of novel type PLA(2) inhibitors is of great interest for both bioorganic studies and clinical application. We focus on designing and synthesizing non - analogues of the phospholipidic substrate of sPLA(2) in order to find new inhibitors. Herein, quinoline - 4 - acetamide sPLA(2) inhibitors were designed by structure - based drug design method and synthesized. The structures of the title compounds were confirmed by elemental analysis, H-1 NMR, IR and MS. The preliminary bioassay data indicated that the title compounds display certain inhibition to sPLA2 at 10 mu mol . L-1 in vitro, and were shown to active on animal model.
关键词[WOS]: PROTEIN
语种: 英语
WOS记录号: WOS:000171884400040
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/139018
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Peking Univ, Inst Chem Phys, State Key Lab Struct Chem Unstable & Stable Speci, Beijing 100871, Peoples R China
2.Peking Univ, Coll Chem & Mol Engn, Beijing 100871, Peoples R China

Recommended Citation:
Liu, Y,Feng, YB,Gao, Y,et al. Structure-based design and synthesis of novel type quinoline as secretory PLA(2) inhibitors[J]. ACTA CHIMICA SINICA,2001,59(10):1751-1755.
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