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琥珀酰亚胺衍生物生物活性研究进展。

Research progress in biological activities of succinimide derivatives.

机构信息

College of Acupuncture & Massage, Shaanxi University of Chinese Medicine, Xixian New Area, Shaanxi Province 712046, PR China; Shaanxi Key Laboratory of Acupuncture & Medicine, Xixian New Area, Shaanxi Province 712046, PR China; School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an 710069, PR China.

Shaanxi Key Laboratory of Acupuncture & Medicine, Xixian New Area, Shaanxi Province 712046, PR China.

出版信息

Bioorg Chem. 2021 Mar;108:104557. doi: 10.1016/j.bioorg.2020.104557. Epub 2020 Dec 15.

Abstract

Succinimides are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have isolated and synthesized succinimide derivatives with multiple medicinal properties including anticonvulsant, anti-inflammatory, antitumor and antimicrobial agents, 5-HT receptor ligands and enzyme inhibitors. Simultaneously, SAR (Structure-Activity Relationship) analysis has been gradually possessed, along with a great deal of derivatives have been derived for potential targets. In this article, we comprehensively summarize the biological activities and SAR for succinimide derivatives, along with the featuring bioactive molecules reported in patents, wishing to provide an overall retrospect and prospect on the succinimide analogues.

摘要

琥珀酰亚胺是药物发现中广泛认可的杂环化合物,在药理学实践中产生了多种治疗相关的应用。药物化学领域的研究已经分离和合成了具有多种药物特性的琥珀酰亚胺衍生物,包括抗惊厥、抗炎、抗肿瘤和抗菌药物、5-HT 受体配体和酶抑制剂。同时,SAR(构效关系)分析逐渐得到了发展,并且为潜在靶点衍生了大量的衍生物。本文全面总结了琥珀酰亚胺衍生物的生物活性和 SAR,以及专利中报道的具有特色的生物活性分子,希望对琥珀酰亚胺类似物进行全面的回顾和展望。

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