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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dc.contributor.authorEgunlusi, Ayodeji, O
dc.contributor.authorMalan, Sarel, F
dc.contributor.authorJoubert, Jacques
dc.date.accessioned2021-09-13T11:24:22Z
dc.date.available2021-09-13T11:24:22Z
dc.date.issued2020-09
dc.description.abstractNeurodegenerative 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.en_US
dc.identifier.urihttps://doi.org/10.24820/ark.5550190.p011.302
dc.identifier.urihttp://hdl.handle.net/10566/6650
dc.language.isoenen_US
dc.publisherArkivocen_US
dc.subject4-Oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneen_US
dc.subjectcycloaddition reactionsen_US
dc.subjectaminolysisen_US
dc.subjectnorbornenesen_US
dc.subjectnorbornene scaffoldsen_US
dc.subjectneurodegenerative disordersen_US
dc.titleSynthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agentsen_US
dc.typeArticleen_US

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