化学
喹啉酮
神经保护
脚手架
组合化学
药理学
计算机科学
程序设计语言
医学
作者
Fan Yang,Wei-Ping He,Jiaqi Yao,Dong Zou,Pu Chen,Jie Li
出处
期刊:Current Organic Synthesis
[Bentham Science]
日期:2019-10-17
卷期号:16 (5): 772-775
被引量:4
标识
DOI:10.2174/1570179416666190328233501
摘要
Objective: To develop efficient method for the synthesis of quinazolinone derivatives bearing different functional groups on ring A and ring B and evaluation as neuroprotective agents. Methods: Synthetic route to quinazolinone derivatives was furnished by condensation/cyclocondensation/ reduction sequence of the activated N-acylbenzotriazoles. The structures of the targets compounds have been deduced upon their spectral data (1HNMR, 13CNMR and Mass spectroscopy). The neuroprotective activities of the synthesized compounds are also evaluated. Results: Preliminary screening on a MPP+ induced SH-SY5Y cell injury model of the synthesized compounds resulted in four compounds (6q, 6r, 6u, and 8e) showed promising neural cell protection activities. The action mechanisms of these compounds on neuroprotection were then analyzed by docking and reverse docking modeling. Conclusion: A series of quinazolinone derivatives, including different substitution types on rings A and B were designed and synthesized via scaffold hopping. With the help of neuroprotective biological evaluation, several efficient therapeutic neuroprotective agents were found for further evaluation as drug candidate against neurodegenerative disorder.
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