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    Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents

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    Egunlusi, Ayodeji O_Synthesis of 4-oxatricyclo[521026]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents_2020.pdf (392.3Kb)
    Date
    2020-09
    Author
    Egunlusi, Ayodeji, O
    Malan, Sarel, F
    Joubert, Jacques
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    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.
    URI
    https://doi.org/10.24820/ark.5550190.p011.302
    http://hdl.handle.net/10566/6652
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