A profound insight into the structural modification of natural bioactive compounds containing piperazine moiety: a comprehensive review..

Q2 Pharmacology, Toxicology and Pharmaceutics Current Bioactive Compounds Pub Date : 2023-07-18 DOI:10.2174/1573407219666230718105347

B. Chopra, N. Saini, Ashwani Kumar Dhingra

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Abstract

Piperazine is the heterocyclic nucleus and exhibits significant biological potential such as antipsychotic, antidepressant, antihistamine, anticancer, anti-anginal, cardioprotective, antiviral, and anti-inflammatory activity. As a result, it had been considered a crucial structural component in the majority of the therapeutic medications that were already on the market. Other issues that limit its use include solubility, limited bioavailability, cost-effectiveness, and a mismatch between the drug's pharmacokinetic and pharmacodynamic profiles. Literature describes structural modification in the piperazine moiety to create novel derivatives or analogues to solve the issues with currently marketed medications. Nature provides various bioactive components having piperazine nuclei in their core structure. The present review describes the potential of the piperazine nucleus present in natural bioactive components. So the study concludes that it is vital to concentrate on the structural characteristics of this scaffold, which opens the way for future research and may benefit pharmaceutical companies as well as medicinal chemists.

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对含哌嗪部分的天然生物活性化合物结构修饰的深刻见解:全面回顾。

哌嗪是杂环核，具有抗精神病、抗抑郁、抗组胺、抗癌、抗心绞痛、心脏保护、抗病毒和抗炎活性等重要的生物学潜力。因此，它被认为是市场上大多数治疗药物的关键结构成分。限制其使用的其他问题包括溶解度、有限的生物利用度、成本效益以及药物的药代动力学和药效学特征之间的不匹配。文献描述了哌嗪部分的结构修饰，以产生新的衍生物或类似物，从而解决当前上市药物的问题。大自然提供了在其核心结构中具有哌嗪核的各种生物活性成分。本综述描述了哌嗪核在天然生物活性成分中的潜力。因此，该研究得出结论，专注于这种支架的结构特征至关重要，这为未来的研究开辟了道路，并可能使制药公司和药物化学家受益。

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来源期刊

Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

1.90

自引率

0.00%

发文量

112

期刊介绍： The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.