Organic and Medicinal Chemistry, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500046, India.
Drug Discov Today. 2013 Apr;18(7-8):389-98. doi: 10.1016/j.drudis.2012.11.003. Epub 2012 Nov 14.
Although a number of anti-inflammatory drugs have been discovered and developed to treat diseases associated with acute and chronic inflammation, many anti-inflammatories cause adverse side effects. The quinoline framework has emerged as a new template for the design and identification of novel anti-inflammatory agents. These agents are classified based on the number of substituents present on the quinoline ring or compounds containing a quinoline ring fused to other heterocycles. This review focuses on the discovery of various quinoline derivatives as inhibitors of cyclooxygenase (COX), phosphodiesterase 4 (PDE4) and tumour necrosis factor-α converting enzyme (TACE), along with transient receptor potential vanilloid 1 (TRPV1) antagonists.
尽管已经发现和开发了许多抗炎药物来治疗与急性和慢性炎症相关的疾病，但许多抗炎药会引起不良反应。喹啉骨架已成为设计和鉴定新型抗炎药物的新模板。这些药物根据喹啉环上存在的取代基的数量或包含与其他杂环稠合的喹啉环的化合物进行分类。本综述重点介绍了各种喹啉衍生物作为环氧化酶 (COX)、磷酸二酯酶 4 (PDE4) 和肿瘤坏死因子-α 转化酶 (TACE) 的抑制剂以及瞬时受体电位香草素 1 (TRPV1) 拮抗剂的发现。
