Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Ghal Kalan, G.T Road, Moga, Punjab, 142001, India.
Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Ghal Kalan, G.T Road, Moga, Punjab, 142001, India.
Eur J Med Chem. 2020 Aug 15;200:112438. doi: 10.1016/j.ejmech.2020.112438. Epub 2020 May 16.
Most of the anti-inflammatory drugs in clinical practice are becoming outdated owing to their potential side and adverse effects. These are found to be highly unsafe for long term use. Thus, since last few years, new anti-inflammatory agents are being developed and number of them are in advanced stages of clinical trials. Heterocyclic molecules have gained great attention of chemists due to their similarity to different biological precursors. In the current review, we have highlighted the recent developments (2015 onwards) in designing and synthesis of various heterocyclic anti-inflammatory molecules along with detailed SAR studies. The principal objective of this review is to provide a profound overview of the recently explored heterocyclic anti-inflammatory agents belonging to various classes such as pyrazole, pyrimidine, benzimidazole, indole, and other related heterocyclic compounds. In addition, an enlarged view on potential interactions of synthetic preparations with target inflammatory enzymes or cytokines has been provided. We have also enlisted lead compounds undergoing different clinical trials against inflammation. The elementary aim of this review is to provide restructured knowledge regarding heterocyclic molecules which will be valuable for the scientists working in the field of anti-inflammatory chemistry. The authors believe that lead compounds mentioned in the report will help to design and develop novel anti-inflammatory drug molecules targeting various factors involved in the progression of inflammation.
由于潜在的副作用和不良反应,大多数临床应用的抗炎药物已经过时。这些药物被发现长期使用极不安全。因此,近年来,人们一直在开发新的抗炎药物,其中一些已经进入临床试验的后期阶段。由于其与不同生物前体的相似性,杂环分子引起了化学家的极大关注。在本次综述中,我们重点介绍了设计和合成各种杂环抗炎分子的最新进展(2015 年以来),以及详细的 SAR 研究。本综述的主要目的是提供对近年来探索的各种类别的杂环抗炎剂的深入概述,如吡唑、嘧啶、苯并咪唑、吲哚和其他相关杂环化合物。此外,还提供了关于合成制剂与靶炎症酶或细胞因子的潜在相互作用的扩展视图。我们还列出了正在进行的针对炎症的不同临床试验的先导化合物。综述的基本目的是提供有关杂环分子的重构知识,这对于从事抗炎化学领域的科学家来说是有价值的。作者认为,报告中提到的先导化合物将有助于设计和开发针对炎症进展中涉及的各种因素的新型抗炎药物分子。