Affiliation:
1. Department of Pharmacy, School of Medicine, Zhejiang University City College, No. 48, Huzhou Road, Hangzhou 310015, Zhejiang, China
Abstract
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.
Funder
Foundation of Hangzhou Science and Technology Information Institute of China
National Science Foundation of China
Publisher
Bentham Science Publishers Ltd.
Subject
Organic Chemistry,Biochemistry
Cited by
5 articles.
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