Products Cited in Publications Worldwide Synthesis and evaluation of 2-methylbenzothiazole derivatives as monoamine oxidase inhibitors

Synthesis and evaluation of 2-methylbenzothiazole derivatives as monoamine oxidase inhibitors

Maryké Shaw; Jacobus P. Petzer; Theunis T. Cloete; Anél Petzer

DOI:

Abstract

Neurodegenerative disorders are caused by the progressive death of neuronal cells in specific regions of the brain and spinal cord. The most common neurodegenerative disorders are Alzheimer’s disease and Parkinson’s disease. The inhibition of enzymes that metabolise amines is an important approach in the treatment of these disorders and B inhibitors have thus been used for the treatment of Parkinson’s disease. Inhibitors of the MAO-A isoform, in turn, are used clinically for the treatment of affective (e.g., major depression) and anxiety disorders. Recent studies have shown that derivatives act as potent inhibitors. Based on these findings, the present study group synthesised thirteen derivatives and evaluated their in vitro inhibition properties. The results showed that the derivatives were potent and selective inhibitors of human MAO-B, with all compounds exhibiting IC50 values < 0.017 µM. The most potent MAO-B inhibitor (4d) had an IC50 value of 0.0046 µM, while the most potent MAO-A inhibitor (5e) had an IC50 value of 0.132 µM. It may be concluded that active derivatives may serve as potential leads for the development of inhibitors for the treatment of neuropsychiatric and neurodegenerative disorders.

Keywords

; ; Parkinson’s disease ; Depression ; ;

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2-Methylbenzo[d]thiazol-6-ol

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2-Methylbenzo[d]thiazol-5-ol

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