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Design, synthesis, and biological activity evaluation of BACE1 inhibitors with antioxidant activity
Author(s) -
Li HeMin,
Yu ShaoPeng,
Fan TianYuan,
Zhong Yue,
Gu Ting,
Wu WenYu,
Zhao Chao,
Chen Zhi,
Chen Min,
Li NianGuang,
Wang XiaoLong
Publication year - 2020
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21585
Subject(s) - antioxidant , abts , dpph , chemistry , enzyme , biochemistry , pharmacology , biological activity , inhibitory postsynaptic potential , in vitro , biology , endocrinology
The proteolytic enzyme β‐secretase (BACE1) plays a central role in the synthesis of the pathogenic β‐amyloid peptides (Aβ) in Alzheimer's disease (AD), antioxidants could attenuate the AD syndrome and prevent the disease progression. In this study, BACE1 inhibitors ( D1 – D18 ) with free radical‐scavenging activities were synthesized by molecular hybridization of 2‐aminopyridine with natural antioxidants. The biological activity evaluation showed that D1 had obvious inhibitory activity against BACE1, and strong antioxidant activity in 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) and 2,2′‐azinobis‐(3‐ethylbenzthiazoline‐6‐sulphonate) (ABTS +• ) assay, which could be used as a lead compound for further study.