Arshdeep Singh, Rabin Debnath, Viney Chawla and Pooja A. Chawla
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引用次数: 0
摘要
高尿酸血症的特点是血液中的尿酸高于正常水平。这种情况会增加患痛风的可能性,痛风是由尿酸盐结晶沉积在关节中引发的一种关节炎,会导致炎症和疼痛。嘌呤代谢的一个重要组成部分是黄嘌呤氧化酶(XO),它将黄嘌呤和次黄嘌呤转化为尿酸。尽管黄嘌呤氧化酶起着至关重要的作用,但痛风等疾病与尿酸水平升高有关,而尿酸水平升高与黄嘌呤氧化酶活性增加有关。为了控制高尿酸血症,本研究重点关注可能作为 XO 抑制剂的潜在氮基杂环化合物,它们可以降低尿酸水平并预防高尿酸血症。黄嘌呤氧化酶抑制剂是一类通过减少尿酸生成来治疗痛风等疾病的药物。本研究展示了许多化合物,特别是含氮杂环化合物,包括它们的合成、结构-活性关系和分子对接研究。本文还包括正在进行临床研究的药物和已获美国食品及药物管理局批准的黄嘌呤氧化酶抑制剂。
Heterocyclic compounds as xanthine oxidase inhibitors for the management of hyperuricemia: synthetic strategies, structure–activity relationship and molecular docking studies (2018–2024)
Hyperuricemia is characterized by higher-than-normal levels of uric acid in the bloodstream. This condition can increase the likelihood of developing gout, a form of arthritis triggered by the deposition of urate crystals in the joints, leading to inflammation and pain. An essential part of purine metabolism is played by the enzyme xanthine oxidase (XO), which transforms xanthine and hypoxanthine into uric acid. Despite its vital role, diseases such as gout have been associated with elevated uric acid levels, which are linked to increased XO activity. To manage hyperuricemia, this study focuses on potential nitrogen based heterocyclic compounds that may serve as XO inhibitors which may lower uric acid levels and prevent hyperuricemia. Xanthine oxidase inhibitors are a class of medications used to treat conditions like gout by reducing the production of uric acid. The present study demonstrates numerous compounds, particularly nitrogen containing heterocyclic compounds including their synthesis, structure–activity relationship, and molecular docking studies. This paper also contains drugs undergoing clinical studies and the xanthine oxidase inhibitors that have been approved by the FDA.
期刊介绍:
Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry.
In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.