Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents
| dc.contributor.author | Egunlusi, Ayodeji O. | |
| dc.contributor.author | Malan, Sarel F. | |
| dc.contributor.author | Joubert, Jacques | |
| dc.date.accessioned | 2021-01-28T07:30:39Z | |
| dc.date.available | 2021-01-28T07:30:39Z | |
| dc.date.issued | 2020 | |
| dc.description.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. | en_US |
| dc.identifier.citation | Egunlusi, A. O. et al. (2020). Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents. Arkivoc ,2020(5) | en_US |
| dc.identifier.issn | 1551-7012 | |
| dc.identifier.uri | 10.24820/ARK.5550190.P011.313 | |
| dc.identifier.uri | http://hdl.handle.net/10566/5784 | |
| dc.language.iso | en | en_US |
| dc.publisher | Arkat USA | en_US |
| dc.subject | Aminolysis | en_US |
| dc.subject | Cycloaddition reactions | en_US |
| dc.subject | Neurodegenerative disorders | en_US |
| dc.subject | Norbornene scaffolds | en_US |
| dc.subject | Norbornenes | en_US |
| dc.title | Synthesis of 4-oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives as lead scaffolds for neuroprotective agents | en_US |
| dc.type | Article | en_US |