Synthesis and Neuroprotective Biological Evaluation of Quinazolinone Derivatives via Scaffold Hopping

Author:

Yang Fan1,He Wei-Ping1,Yao Jia-Qi1,Zou Dong1,Chen Pu1,Li Jie1

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

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