Design, synthesis and biological evaluation of novel chiral oxazino-indoles as potential and selective neuroprotective agents against Aβ25–35-induced neuronal damage. Issue 15 (1st August 2016)

• Record Type: Journal Article
• Authors: Chen, Jing; Tao, Ling-Xue; Xiao, Wei; Ji, Sha-Sha; Wang, Jian-Rong; Li, Xu-Wen; Zhang, Hai-Yan; Guo, Yue-Wei
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 15(2016)
• Page Start: 3765
• Page End: 3769
• Publication Date: 2016-08-01
• Subjects: Oxazino-indoles -- Oxa-Pictet–Spengler reaction -- Neuroprotective agent -- Alzheimer's disease -- SAR; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.061
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of chiral oxazino-indoles have been synthesized via a key intermolecular oxa-Pictet–Spengler reaction. These compounds exhibited significant and selective neuroprotective effects against Aβ25–35 -induced neuronal damage. This is the first report of evaluating the influence of chiral diversity of oxazino-indoles on their neuroprotective activities, with the structure–activity relationship been analyzed. The highly active compounds3f, 3g, 4g, 4h, and6b all performed over 90% cell protection, providing a new direction for the development of neuroprotective agents against Alzheimer's disease.