Novel tricycloundecane derivatives as potential N-methyl-Daspartate receptor and calcium channel inhibitors for neuroprotection
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Date
2014
Authors
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Journal ISSN
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Publisher
University of the Western Cape
Abstract
This study focused on the synthesis of a series of novel tricycloundecane derivatives and evaluation of these compounds for neuroprotection using the fluorescent ratiometric calcium assay that indicates the ability of the test compounds to inhibit NMDA receptors and VGCC. The cycloaddition reaction between p-benzoquinone and monomerised dicyclopentadiene yielded tricycloundeca- 4,9-diene-3,6-dione which was used as the base structure and further derivatised. These derivatives were conjugated with benzylamine to form a series of imines and amines. A total of 10 compounds were synthesised for evaluation of inhibition of calcium influx through NMDA receptor channels and voltage-gated calcium channels. The structures were confirmed using NMR, IR and MS. On the proton NMR, the characteristic AB-quartet system was observed in the region of 1-2 ppm for all the compounds and the aromatic moiety was observed between 6.5-7.5 ppm for the novel polycyclic amines. These, with other functional groups, were used to confirm the individual structures
Description
>Magister Scientiae - MSc
Keywords
Neurodegenerative disorders, Tricycloundecane, N-methyl-D-aspartate receptor, Voltage-gated calcium channel, Oxidative stress, Synaptoneurosomes, Excitotoxicity, Apoptosis, Necrosis, Polycyclic cage, Neuroprotective agents, Fura-2 AM