Synthesis and biological evaluation of 3-carbamate smilagenin derivatives as potential neuroprotective agents

被引：6

作者：

Zhang, Cong ^{[1
]}

Wu, Yan ^{[1
]}

Li, Jie ^{[1
]}

Yang, Gui-Xiang ^{[1
]}

Su, Lin ^{[1
]}

Huang, Yan ^{[1
]}

Wang, Rui ^{[1
]}

Ma, Lei ^{[1
]}

机构：

[1] East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, 130 Meilong Rd, Shanghai 200237, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 19期

基金：

中国国家自然科学基金;

关键词：

Smilagenin derivatives; Alzheimer's disease; Oxidative stress; Neuroprotective activity; SARSASAPOGENIN DERIVATIVES; NEUROTROPHIC FACTOR; ALZHEIMERS-DISEASE; DESIGN; DAMAGE; CELLS;

D O I：

10.1016/j.bmcl.2019.08.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Studies indicated that smilagenin, isolated from Anemarrhena asphodeloides Bunge, could improve cognitive impairment and exhibit neuroprotective activity. On the basis of the structure of smilagenin, a series of derivatives were synthesized and evaluated for their neuroprotective effects of H2O2-induced, oxygen glucose deprivation-induced neurotoxicity in SH-SY5Y cells and LPS-induced NO production in RAW264.7 cells. Structure activity relationship of derivatives revealed that benzyl-substituted piperazine formate derivatives showed the potent neuroprotective activity such as A12. These findings may provide new insights for the development of neuroprotective agents against Alzheimer's disease.

引用

页数：5

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