Belinda Strydom

Monoamine oxidase, especially monoamine oxidase 8 (MAO-8), plays a major role in the therapy of Parkinson's disease (PO). MAO-8 is the main enzyme responsible for the catabolism of dopamine in the substantia nigra of the brain. Inhibition of MAO-8 may thus conserve dopamine in the brain and provide symptomatic relief to PO patients. MAO inhibitors are currently being studied as a treatment strategy for neurodegenerative diseases such as PD. In addition to symptomatic relief, MAO inhibitors are also thought to have neuroprotective properties and may slow the neurodegenerative process and thus the progress of the disease. The most common MAO-8 inhibitor used for the treatment of PO is selegiline [(R)-deprenyl], an irreversible inhibitor. Unfortunately, selegiline has psycotoxic and cardiovascular adverse effects due to amphetamine me;tabolites formed during its oxidation. This justifies the need for the development of novel, safe and reversible MAO-8 inhibitors for the treatment ...

vi side chains on C6. To investigate the importance of the oxy moiety for MAO inhibitory activity, the effects of benzylamino substitution on the C6 position of the phthalide ring was also examined. The alkyloxyphthalide analogues were synthesized by reacting 6-hydroxyphthalide with an appropriately substituted alkyl bromide. The benzylaminophthalide was synthesized, in turn, according to the same procedure from 6-aminophthalide and benzyl bromide. The synthesized compounds were evaluated as inhibitors of recombinant human MAO-A and –B. Kynuramine, a MAO-A/B mixed substrate served as enzyme substrate. Kynuramine is oxidized by the MAOs to yield 6-hydroxyquinoline, a compound which fluoresces in alkaline media. Concentration measurements of 6hydroxyquinoline can conveniently be made via fluorescence spectrophotometry since both kynuramine and the inhibitors are non-fluorescent under these assay conditions. The inhibition potencies of the test compounds were expressed as the correspon...

Monoamine oxidase, especially monoamine oxidase 8 (MAO-8), plays a major role in the therapy of Parkinson's disease (PO). MAO-8 is the main enzyme responsible for the catabolism of dopamine in the substantia nigra of the brain. Inhibition of MAO-8 may thus conserve dopamine in the brain and provide symptomatic relief to PO patients. MAO inhibitors are currently being studied as a treatment strategy for neurodegenerative diseases such as PD. In addition to symptomatic relief, MAO inhibitors are also thought to have neuroprotective properties and may slow the neurodegenerative process and thus the progress of the disease. The most common MAO-8 inhibitor used for the treatment of PO is selegiline [(R)-deprenyl], an irreversible inhibitor. Unfortunately, selegiline has psycotoxic and cardiovascular adverse effects due to amphetamine me;tabolites formed during its oxidation. This justifies the need for the development of novel, safe and reversible MAO-8 inhibitors for the treatment o...

There are currently various initiatives in the South African health sector aimed at increasing patient access to medication. The National Department of Health’s (NDoH’s) National Adherence Strategy is one such initiative, which provides alternative options for dispensing to and collection of medication by patients who have been prescribed chronic medication.