This review brings together the various pathways to the oxazino[4,3-a]indole motif over the last decades. Representative examples showing the scope of these processes will illustrate the synthetic pathways and the biological activity of the synthesized oxazinoindoles will be mentioned wherever possible.
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| http://dx.doi.org/10.1016/j.ejmech.2021.113728 | DOI Listing |
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Design, synthesis and biological evaluation of novel chiral oxazino-indoles as potential and selective neuroprotective agents against Aβ25-35-induced neuronal damage.
Bioorg Med Chem Lett
August 2016
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, PR China. Electronic address:
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.
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