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Coumarin-piperazine derivatives as biologically active compounds

机译:香豆素-哌嗪衍生物为生物活性化合物

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摘要

A number of psychiatric disorders, including anxiety, schizophrenia, Parkinson’s disease, depression and others CNS diseases are known to induce defects in the function of neural pathways sustained by the neurotransmitters, like dopamine and serotonin. -arylpiperazine moiety is important for CNS-activity, particularly for serotonergic and dopaminergic activity. In the scientific literature there are many examples of coumarin-piperazine derivatives, particularly with arylpiperazines linked to a coumarin system via an alkyl liner, which can modulate serotonin, dopamine and adrenergic receptors. Numerous studies have revealed that the inclusion of a piperazine moiety could occasionally provide unexpected improvements in the bioactivity of various biologically active compounds. The piperazine analogs have been shown to have a potent antimicrobial activity and they can also act as BACE-1 inhibitors. On the other hand, arylpiperazines linked to coumarin derivatives have been shown to have antiproliferative activity against leukemia, lung, colon, breast, and prostate tumors. Recently, it has been reported that coumarin-piperazine derivatives exhibit a Fneuroprotective effect by their antioxidant and anti-inflammatory activities and they also show activity as acetylcholinesterase inhibitors and antifilarial activity. In this work we provide a summary of the latest advances in coumarin-related chemistry relevant for biological activity.
机译:已知许多精神疾病,包括焦虑症,精神分裂症,帕金森氏病,抑郁症和其他中枢神经系统疾病,都会诱发由神经递质(如多巴胺和5-羟色胺)维持的神经通路功能的缺陷。 -芳基哌嗪部分对于CNS活性特别是对于血清素能和多巴胺能活性是重要的。在科学文献中,有许多香豆素-哌嗪衍生物的实例,特别是芳基哌嗪通过烷基内衬与香豆素系统相连,该烷基衬里可以调节5-羟色胺,多巴胺和肾上腺素能受体。大量研究表明,哌嗪部分的加入有时会在各种生物活性化合物的生物活性方面提供意想不到的改善。已经显示哌嗪类似物具有有效的抗菌活性,它们也可以作为BACE-1抑制剂。另一方面,已显示与香豆素衍生物连接的芳基哌嗪具有抗白血病,肺,结肠,乳腺和前列腺肿瘤的抗增殖活性。近来,已经报道了香豆素-哌嗪衍生物通过其抗氧化剂和抗炎活性显示出神经保护作用,并且它们还显示出作为乙酰胆碱酯酶抑制剂的活性和抗丝活性。在这项工作中,我们总结了与生物活性有关的香豆素相关化学的最新进展。

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