1,2,4-三唑和1,3,4-噻二唑衍生物作为潜在的麻醉和抗炎剂的综述

Q3 Pharmacology, Toxicology and Pharmaceutics
Andriy Koval, A. Lozynskyi, S. Shtrygol’, R. Lesyk
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引用次数: 3

摘要

的目标。本文综述了三唑和噻二唑类杂环化合物在生物有机化学和药物化学中的合成和结构修饰研究进展。材料和方法。本研究以文献语义学和分析方法为基础,利用书目数据库和摘要数据库以及化合物数据库进行研究。结果。现代药物化学面临着许多挑战,其中之一是治疗剂的活性和特异性的确定。最近的科学数据表明,三唑类和/或噻二唑类具有广泛的生物活性,特别是抗菌、抗真菌、抗病毒、抗癌和抗惊厥。合成研究为生物活性三唑和/或噻二唑衍生物的分子设计提出了许多新的方向,并获得了包含数百种新化合物的定向文库。本文综述了近十年来其镇痛和抗炎活性的数据。我们总结和分析了一系列的三唑和/或噻二唑衍生物,并提供了它们的构效关系数据。为了优化和合理设计具有最佳“类药”特性的高活性分子,发现可能的SAR作用机制,本文对QSAR分析和分子对接进行了总结。结论。含有三唑和/或噻二唑片段的杂环系统是有前途的镇痛和/或抗炎剂的重要来源。结果表明,上述杂环衍生物的作用选择性高,毒性低,效果与标准药物相当
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An overview on 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential anesthesic and anti-inflammatory agents
The aim. The purpose of this review is to summarize data on the synthesis and structural modification of heterocyclic systems with triazole and thiadiazole fragments in molecules as promising objects in bioorganic and medicinal chemistry. Materials and methods. The research based on bibliosemantic and analytical methods using bibliographic and abstract databases, as well as databases of chemical compounds. Results. Modern medicinal chemistry faces many challenges, one of which is the determination of the activity and specificity of therapeutic agents. Recent scientific data showed that triazoles and/or thiadiazoles have broad spectrum of biological activities, in particular antimicrobial, antifungal, antiviral, anticancer and anticonvulsant. Synthetic research allows to propose a whole number of new molecular design directions of biological active triazole and/or thiadiazole derivatives, as well as to obtain directed library that include hundreds of new compounds. This review is an effort to summarize data of its analgesic and anti-inflammatory activity over the last decade. We summarized and analyzed the series of triazole and/or thiadiazole derivatives and provided data of their structure-activity relationship. For optimization and rational design of highly active molecules with optimal «drug-like» characteristics and discovering of possible mechanism of action SAR, QSAR analysis and molecular docking were summarized. Conclusions. It has been shown that heterocyclic systems containing fragments of triazole and / or thiadiazole are a significant source of promising analgesic and/or anti-inflammatory agents. It has been established that the mentioned heterocyclic derivatives have a high selectivity of action, low toxicity and an effect commensurate with standard drugs
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来源期刊
ScienceRise: Pharmaceutical Science
ScienceRise: Pharmaceutical Science Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.70
自引率
0.00%
发文量
39
审稿时长
6 weeks
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