Synthesis and decreasing Aβ content evaluation of arctigenin-4-yl carbamate derivatives. Issue 13 (1st July 2016)

• Record Type: Journal Article
• Authors: Xu, Xingyu; Li, Cong; Lei, Min; Zhu, Zhiyuan; Yan, Jianming; Shen, Xu; Hu, Lihong
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 13(2016)
• Page Start: 2988
• Page End: 2991
• Publication Date: 2016-07-01
• Subjects: Arctigenin (ATG) -- Natural product -- Arctigenin-4-yl 3-carbamate -- Structure–activity relationships (SARs) -- Alzheimer's disease (AD); Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.028
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of arctigenin-4-yl carbamate derivatives were synthesized and evaluated for potency in reducing β -amyloid (A β ) content in HEK293-APPswe cells. Most of the arctigenin-4-yl aralkyl or aryl carbamate derivatives showed improved potency in reducing A β content. Among the synthesized compounds, arctigenin-4-yl (3-chlorophenyl)carbamate (20 ) exhibited the strongest potency with 78.7% A β content reduction at 20 μM. Furthermore, the effect of arctigenin-4-yl (4-chlorophenyl)carbamate (19 ) and arctigenin-4-yl (3-chlorophenyl)carbamate (20 ) on lowing A β content was better than arctigenin under the concentrations of 1, 10 and 20 μM.