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芳基哌嗪衍生物作为治疗各种神经障碍的潜在治疗药物的综述。

A Review on the Arylpiperazine Derivatives as Potential Therapeutics for the Treatment of Various Neurological Disorders.

机构信息

Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, Punjab- 151401, India.

Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GhalKalan, G.T. Road, Moga, Punjab 142001, India.

出版信息

Curr Drug Targets. 2022;23(7):729-751. doi: 10.2174/1389450123666220117104038.

Abstract

Neurological disorders are disease conditions related to the neurons and central nervous system (CNS). Any structural, electrical, biochemical, and functional abnormalities in neurons can lead to various types of disorders, like Alzheimer's disease (AD), depression, Parkinson's disease (PD), epilepsy, stroke, etc. Currently available medicines are symptomatic and do not treat the disease state. Thus, novel CNS active agents with the potential to completely treat an illness are highly desired. A range of small organic molecules is being explored as potential drug candidates to cure different neurological disorders. In this context, arylpiperazinehas been found to be a versatile scaffold and indispensable pharmacophore in many CNS active agents. Several molecules with arylpiperazine nucleus have been developed as potent leads for the treatment of AD, PD, depression, and other disorders. The arylpiperazine nucleus can be optionally substituted at different chemical structures and offer flexibility for the synthesis of a large number of derivatives. In the current review article, we have explored the role of various arylpiperazine containing scaffolds against different neurological disorders, including AD, PD, and depression. The structure-activity relationship studies were conducted for recognizing potent lead compounds. This review article may provide important insights into the structural requirements for designing and synthesizing effective molecules as curative agents for different neurological disorders.

摘要

神经紊乱是与神经元和中枢神经系统(CNS)相关的疾病状况。神经元的任何结构、电、生化和功能异常都可能导致各种类型的紊乱,如阿尔茨海默病(AD)、抑郁症、帕金森病(PD)、癫痫、中风等。目前可用的药物是对症治疗,不能治疗疾病状态。因此,人们非常希望有新型的、具有治疗潜力的中枢神经系统活性药物。目前正在探索一系列小分子有机化合物作为治疗不同神经紊乱的潜在药物候选物。芳基哌嗪已被发现是许多中枢神经系统活性药物中的多功能支架和不可或缺的药效团。已经开发出几种含有芳基哌嗪核的分子作为治疗 AD、PD、抑郁症和其他疾病的有效先导化合物。芳基哌嗪核可以在不同的化学结构上进行可选取代,为合成大量衍生物提供了灵活性。在当前的综述文章中,我们探讨了含有各种芳基哌嗪结构的支架在不同神经紊乱中的作用,包括 AD、PD 和抑郁症。我们进行了构效关系研究,以识别有效的先导化合物。这篇综述文章可能为设计和合成有效分子作为不同神经紊乱治疗药物提供重要的结构要求方面的见解。

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