Design and synthesis of nitrogen-fused pyridazinone fluorescent probes and their application in biological imaging  

氮杂芳香环并哒嗪酮类荧光探针的设计、合成和生物成像的应用（英文）

作　　者：Hui Liu Lei Liang Lan Yuan Fengrong Xu Yan Niu Chao Wang Ping Xu 刘慧;梁磊;袁兰;许凤荣;牛彦;王超;徐萍(北京大学医学部药学院药物化学系,北京100191;北京大学医药卫生分析中心,北京100191)

机构地区：[1]Department of Medicinal Chemisry,School oPharmaceutical Sciences,Peking Uiniversity Healih Science Center,Beijing 100191,China [2]Medical and Healthy Analysis Center,Peking University,Beijing 100191,China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2019年第5期298-315,共18页中国药学（英文版）

基　　金：Beijing Natural Science Foundation(Grant No.7162110);Interdisciplinary Medicine Seed Fund of Peking University(Grant No.BMU2018MC004);the National Natural Science Foudation of China(Grant No.201807006,81872731,91630314)

摘　　要：A series of small-molecular fluorescent probes based on nitrogen-fused pyridazinone scaffold were developed in this report.The design strategy involved two steps:1)enhancing the electron-withdrawing ability of the acceptor by incorporating an N-heterocyclic aromatic ring(pyridine or pyrazine)at the C4 and C5 positions of the pyridazinone skeleton and 2)anchoring a triphenylphosphine or morpholine tail as the subcellular targeting group.These fluorescent probes displayed excellent properties in live cell and brain tissue imaging.本文合成了一系列氮杂芳香环并哒嗪酮的小分子荧光探针。设计策略主要包括以下两点:1)通过在哒嗪酮4, 5-C上并入含氮芳香杂环(吡啶或吡嗪),增强电子受体的吸电子能力; 2)末端引入细胞器靶向基团三苯基膦或吗啡啉。这些探针在活细胞成像和脑组织成像上均表现出优良的性质。

关 键 词：Nitrogen-fused pyridazinone Fluorescent probe Biological imaging DESIGN SYNTHESIS 

分 类 号：R916[医药卫生—药学]