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 neurotransmitter amines is an important approach in the treatment of these disorders and monoamine oxidase (MAO) 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 benzothiazole derivatives act as potent MAO inhibitors. Based on these findings, the present study group synthesised thirteen 2-methylbenzo[d]thiazole derivatives and evaluated their in vitro MAO inhibition properties. The results showed that the benzothiazole 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 benzothiazole derivatives may serve as potential leads for the development of MAO inhibitors for the treatment of neuropsychiatric and neurodegenerative disorders.

神经退行性疾病是由大脑和脊髓特定区域的神经元细胞进行性死亡引起的。最常见的神经退行性疾病是阿尔茨海默病和帕金森病。抑制神经递质胺代谢酶是治疗这些疾病的重要方法，因此单胺氧化酶 (MAO) B 抑制剂已用于治疗帕金森病。 MAO-A 亚型抑制剂又在临床上用于治疗情感障碍（例如重度抑郁症）和焦虑症。最近的研究表明，苯并噻唑衍生物可作为有效的 MAO 抑制剂。基于这些发现，本研究小组合成了13种2-甲基苯并[d]噻唑衍生物，并评估了它们的体外MAO抑制特性。结果表明，苯并噻唑衍生物是人 MAO-B 的有效且选择性抑制剂，所有化合物的 IC ₅₀ 值 < 0.017 µM。最有效的 MAO-B 抑制剂 (4d) 的 IC ₅₀ 值为 0.0046 µM，而最有效的 MAO-A 抑制剂 (5e) 的 IC ₅₀ 值为 0.132 µM 。可以得出结论，活性苯并噻唑衍生物可以作为开发用于治疗神经精神和神经退行性疾病的 MAO 抑制剂的潜在先导。