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一种基于NBD胺硫解作用的荧光HS触发前药。

A fluorogenic HS-triggered prodrug based on thiolysis of the NBD amine.

作者信息

Xie Yonghui, Huang Haojie, Ismail Ismail, Sun Hongyan, Yi Long, Xi Zhen

机构信息

State Key Laboratory of Elemento-Organic Chemistry and Department of Chemical Biology, National Engineering Research Center of Pesticide (Tianjin), College of Chemistry, Nankai University, Tianjin 300071, China.

State Key Laboratory of Organic-Inorganic Composites and Beijing Key Laboratory of Bioprocess, Beijing University of Chemical Technology (BUCT), Beijing 100029, China.

出版信息

Bioorg Med Chem Lett. 2019 Oct 1;29(19):126627. doi: 10.1016/j.bmcl.2019.126627. Epub 2019 Aug 17.

DOI:10.1016/j.bmcl.2019.126627
PMID:31444083
Abstract

Based on thiolysis of the NBD amine, a HS-triggered prodrug has been designed and synthesized for localized production of ciprofloxacin under micromolar HS. Activation of the prodrug can be monitored through fluorescence in real-time. We envision that thiolysis of the NBD amine could be readily used for development of other HS-triggered prodrugs in the future.

摘要

基于NBD胺的硫解反应,设计并合成了一种由HS触发的前药,用于在微摩尔浓度的HS条件下局部产生环丙沙星。前药的活化可通过荧光进行实时监测。我们设想,NBD胺的硫解反应未来可很容易地用于开发其他由HS触发的前药。

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引用本文的文献

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NBD-based synthetic probes for sensing small molecules and proteins: design, sensing mechanisms and biological applications.基于 NBD 的小分子和蛋白质的合成探针:设计、传感机制和生物应用。
Chem Soc Rev. 2021 Jul 5;50(13):7436-7495. doi: 10.1039/d0cs01096k.
2
A Fast-Response Red Shifted Fluorescent Probe for Detection of HS in Living Cells.一种用于检测活细胞中 HS 的快速响应红移荧光探针。
Molecules. 2020 Jan 21;25(3):437. doi: 10.3390/molecules25030437.