布洛芬衍生物的合成策略:分类研究。

IF 2.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Current topics in medicinal chemistry Pub Date : 2025-01-10 DOI:10.2174/0115680266334717241127043711
Kuchana Madhavi, Barla Karuna Devi
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引用次数: 0

摘要

布洛芬是一种广泛使用的芳基丙酸类非甾体抗炎药,能有效缓解疼痛、发烧和炎症。长期使用可导致胃肠道、肝脏和肾脏毒性,特别是胃肠道溃疡。这些副作用很大程度上归因于非甾体抗炎药常见的羧酸官能团。本综述重点介绍了不同的研究人员对布洛芬中羧基的不同修饰,如酯、酰胺、羟肟酸和n -取代肼,以及杂环部分如三唑、四唑和恶二唑的整合。此外,布洛芬已与其他药物杂交,并与金属络合,以提高治疗效果。不同的合成策略是采用酯化,酰胺化,缩合,希夫碱形成等。这些修饰产生了具有抗菌、抗真菌、抗癌和其他生物活性的衍生物,旨在减少副作用,同时保留或增强抗炎、镇痛和解热特性。
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Synthetic Strategies for the Development of Ibuprofen Derivatives: A Classified Study.

Ibuprofen, a widely used NSAID from the aryl propionic acid class, effectively relieves pain, fever, and inflammation. On prolonged use, it leads to gastrointestinal, hepatic, and renal toxicities, particularly gastrointestinal ulcers. These side effects are largely attributed to the carboxylic acid functional group common to NSAIDs. The present review highlights the different modifications done to the carboxylic group in Ibuprofen, by various researchers such as esters, amides, hydroxamic acids, and N-substituted hydrazides, along with the integration of heterocyclic moieties like triazoles, tetrazoles, and oxadiazoles. Additionally, Ibuprofen has been hybridized with other drugs and complexed with metals to enhance therapeutic effects. The different synthetic strategies that were employed were esterification, amidation, condensation, Schiff’s base formation, etc. These modifications have resulted in derivatives with antimicrobial, antifungal, anticancer, and other biological activities, aiming to reduce side effects while retaining or enhancing anti-inflammatory, analgesic, and antipyretic properties.

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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
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