作者
Zahra Haghighijoo, Omidreza Firuzi, Bahram Hemmateenejad, Saeed Emami, Najmeh Edraki, Ramin Miri
发表日期
2017/10/1
期刊
Bioorganic Chemistry
卷号
74
页码范围
126-133
出版商
Academic Press
简介
Discovering multifunctional agents for the treatment of Alzheimer’s disease (AD) is an attractive therapeutic approach. BACE1 (β-site amyloid precursor protein cleaving enzyme 1) inhibitors may play a pivotal role in treating AD. Therefore, the discovery of novel non-peptide BACE1 inhibitors with desirable blood brain barrier permeability is a favorable approach for treatment. Moreover, the antioxidant potential of a drug could serve as an added value for designing dual-acting therapeutic agents. Here, we report the design, synthesis and biological evaluation of quinazolinone-hydrazone derivatives as new multi-target candidates for the treatment of AD. The compounds were investigated for their in vitro BACE1 inhibitory potential using a FRET-based enzymatic assay and also screened for antioxidant activity using DPPH. Among them, compound 4h bearing a 2,3-dichlorophenyl moiety showed the highest activity …
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Z Haghighijoo, O Firuzi, B Hemmateenejad, S Emami… - Bioorganic Chemistry, 2017