Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents
Loading...
Date
2020
Authors
Journal Title
Journal ISSN
Volume Title
Publisher
ARKAT USA
Abstract
Neurodegenerative disorders are characterised by progressive loss of neuronal functions. Of the proposed mechanisms, excitotoxicity, mediated by prolonged glutamate activation and calcium overload, is prominent. NGP1-01, a polycyclic cage amine, and tricyclo[6.2.1.02,7]undec-9-ene-3,6-dione have been shown to display calcium-modulating properties. In this study, we synthesised structurally-related 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione as the base scaffold, and incorporated various functional moieties through aminolysis, to afford a series of imide derivatives. All final compounds were obtained in yields between 47-97% and their structures were confirmed by NMR, IR and MS. These structurally-related derivatives could potentially act as neuroprotective agents. Additionally, their synthetic versatilities could make them precursors, as lead compounds, to potential pharmacologically-active agents.
Description
Keywords
4-Oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione, Cycloaddition reactions, Aminolysis, Norbornenes, Norbornene scaffolds, Neurodegenerative disorders
Citation
Egunlusi, Ayodeji & Malan, Sarel & Joubert, Jacques. (2020). Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents. 10.24820/ark.5550190.p011.302.