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Agents for the Treatment of Gout: Current Advances and Future Perspectives
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2023-10-31 , DOI: 10.1021/acs.jmedchem.3c01710 Xiaoyi Zeng 1 , Yajing Liu 1 , Yuxin Fan 1 , Di Wu 1 , Yangyang Meng 1 , Mingze Qin 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2023-10-31 , DOI: 10.1021/acs.jmedchem.3c01710 Xiaoyi Zeng 1 , Yajing Liu 1 , Yuxin Fan 1 , Di Wu 1 , Yangyang Meng 1 , Mingze Qin 1
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Gout is characterized by hyperuricemia and the deposition of monosodium urate (MSU) crystals around joints. Despite the availability of several drugs on the market, its treatment remains challenging owing to the notable side effects, such as hepatorenal toxicity and cardiovascular complications, that are associated with most existing agents. This perspective aims to summarize the current research progress in the development of antigout agents, particularly focusing on xanthine oxidase (XO) and urate anion transporter 1 (URAT1) inhibitors from a medicinal chemistry viewpoint and their preliminary structure–activity relationships (SARs). This perspective provides valuable insights and theoretical guidance to medicinal chemists for the discovery of antigout agents with novel chemical structures, better efficiency, and lower toxicity.
中文翻译：
痛风治疗药物：当前进展和未来展望
痛风的特征是高尿酸血症和关节周围单钠尿酸盐 (MSU) 晶体的沉积。尽管市场上有多种药物可供使用，但由于与大多数现有药物相关的显着副作用，例如肝肾毒性和心血管并发症，其治疗仍然具有挑战性。本视角旨在总结当前抗痛风药物开发的研究进展，特别是从药物化学角度重点关注黄嘌呤氧化酶（XO）和尿酸阴离子转运蛋白1（URAT1）抑制剂及其初步构效关系（SAR）。这一观点为药物化学家发现化学结构新颖、效率更高、毒性更低的抗痛风药物提供了宝贵的见解和理论指导。
更新日期：2023-10-31
中文翻译：
痛风治疗药物：当前进展和未来展望
痛风的特征是高尿酸血症和关节周围单钠尿酸盐 (MSU) 晶体的沉积。尽管市场上有多种药物可供使用，但由于与大多数现有药物相关的显着副作用，例如肝肾毒性和心血管并发症，其治疗仍然具有挑战性。本视角旨在总结当前抗痛风药物开发的研究进展，特别是从药物化学角度重点关注黄嘌呤氧化酶（XO）和尿酸阴离子转运蛋白1（URAT1）抑制剂及其初步构效关系（SAR）。这一观点为药物化学家发现化学结构新颖、效率更高、毒性更低的抗痛风药物提供了宝贵的见解和理论指导。
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