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A Comprehensive review of Monoamine Oxidase-A Inhibitors in Their Syntheses and Potencies.
Combinatorial Chemistry & High Throughput Screening ( IF 1.6 ) Pub Date : 2020-10-31 , DOI: 10.2174/1386207323666200428091306
Nisha A Rehuman 1 , Bijo Mathew 2 , Rakesh K Jat 1 , Orazio Nicolotti 3 , Hoon Kim 4
Affiliation  

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.



中文翻译:

单胺氧化酶-A抑制剂的合成和效力的全面审查。

背景:单胺氧化酶(MAO)在各种神经退行性疾病的发展过程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,与线粒体外膜结合并催化5-羟色胺,去甲肾上腺素和多巴胺等神经递质的氧化转化。

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,并且组合和平行合成的发展加快了合成方案的发展。在这里,我们提供了用于制备不同类别的MAO-A抑制剂的合成方案的概述。我们根据这些抑制剂的分子支架和所用的合成方法对其进行分类。

结果:报告了来自不同类别的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。

更新日期:2020-12-22
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