oa SA Pharmaceutical Journal - Novel sulfanyl- and sulfinylcaffeine analogues as inhibitors of monoamine oxidase : cum laude
Parkinson's disease is a neurodegenerative disorder which is progressive in nature and is characterised by motor disturbances, such as bradykinesia and muscular rigidity. It is normally associated with the elderly and leads to reduced life quality.
These disturbances are due to degeneration of the dopaminergic neurons that originate in the substantia nigra pars compacta (SNpc), with the subsequent loss of their terminals in the striatum. It differs to normal loss thereof due to ageing. This degenerative process leads to the depletion of the dopamine that is normally found in SNpc neurons. The monoamine oxidases, MAO-A and MAO-B, are mitochondrial outer-membrane-bound flavin adenine dicnucleotide- (FAD) containing enzymes responsible for oxidation of dopamine in the human brain. Therefore, inhibitors of MAO-A and MAO-B may reduce the central catabolism of dopamine, and thus provide relief from the symptoms of Parkinson's disease. Inthis study, novel inhibitors of MAO-A and MAO-B were designed and synthesised in an attempt to discover new anti-parkinsonian drugs.
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