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单胺氧化酶-A 抑制剂的合成与效能的综合评价

A Comprehensive Review of Monoamine Oxidase-A Inhibitors in their Syntheses and Potencies.

机构信息

Department of Pharmaceutical Chemistry, JJTU University, Jhunjhunu, India.

Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, Amrita Health Science Campus, Kochi-682, India.

出版信息

Comb Chem High Throughput Screen. 2020;23(9):898-914. doi: 10.2174/1386207323666200428091306.

Abstract

BACKGROUND

Monoamine oxidases (MAOs) play a crucial role during the development of various neurodegenerative disorders. There are two MAO isozymes, MAO-A and MAO-B. MAO-A is a flavoenzyme, which binds to the outer mitochondrial membrane and catalyzes the oxidative transformations of neurotransmitters like serotonin, norepinephrine, and dopamine.

MATERIALS AND METHODS

Focus on synthetic studies has culminated in the preparation of many MAOA inhibitors, and advancements in combinatorial and parallel synthesis have accelerated the developments of synthetic schemes. Here, we provided an overview of the synthetic protocols employed to prepare different classes of MAO-A inhibitors. We classified these inhibitors according to their molecular scaffolds and the synthetic methods used.

RESULTS

Various synthetic and natural derivatives from a different class of MAO-A inhibitors were reported.

CONCLUSION

The review provides a valuable tool for the development of a new class of various selective MAO-A inhibitors for the treatment of depression and other anxiety disorders.

摘要

背景

单胺氧化酶(MAO)在各种神经退行性疾病的发展中起着至关重要的作用。有两种 MAO 同工酶,MAO-A 和 MAO-B。MAO-A 是一种黄素酶,它与外线粒体膜结合,并催化神经递质如血清素、去甲肾上腺素和多巴胺的氧化转化。

材料和方法

对合成研究的关注最终导致了许多 MAOA 抑制剂的制备,组合和并行合成的进步加速了合成方案的发展。在这里,我们提供了用于制备不同类别的 MAO-A 抑制剂的合成方案概述。我们根据它们的分子支架和使用的合成方法对这些抑制剂进行了分类。

结果

报道了来自不同类别的 MAO-A 抑制剂的各种合成和天然衍生物。

结论

该综述为开发用于治疗抑郁症和其他焦虑症的新型各种选择性 MAO-A 抑制剂提供了有价值的工具。

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