Xie Yonghui, Huang Haojie, Ismail Ismail, Sun Hongyan, Yi Long, Xi Zhen
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.
Bioorg Med Chem Lett. 2019 Oct 1;29(19):126627. doi: 10.1016/j.bmcl.2019.126627. Epub 2019 Aug 17.
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.
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。