Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, China.
Department of Molecular Microbiology and Immunology, Saint Louis University School of Medicine, St. Louis, MO, USA; Saint Louis University Liver Center, Saint Louis University School of Medicine, St. Louis, MO, USA.
Eur J Med Chem. 2020 Nov 15;206:112714. doi: 10.1016/j.ejmech.2020.112714. Epub 2020 Aug 5.
Hepatitis B is a vaccine-preventable, but potentially life-threatening liver infection caused by the Hepatitis B virus (HBV). It represents an important health burden, with 257 million active cases globally. Current HBV treatments using nucleos(t)ide analogs and pegylated interferons cannot alleviate the situation completely since they are unable to cure the infection or reduce the amount of viral covalently closed circular DNA (cccDNA). The HBV core protein is a small protein of 183 amino acids that participates in multiple essential functions in the HBV replicative cycle. Capsid assembly modulators that target the core protein are being developed. Sulfonamides are synthetic functional groups, found in several drugs. Herein, we provide a concise report focusing on the sulfamoylbenzamides as HBV capsid modulators, and medicinal chemistry strategies used in their design and development.
乙型肝炎是一种由乙型肝炎病毒（HBV）引起的、可通过疫苗预防但可能危及生命的肝脏感染。它是一个重要的健康负担，全球有 2.57 亿例活跃病例。目前使用核苷酸类似物和聚乙二醇干扰素的 HBV 治疗方法并不能完全缓解这种情况，因为它们不能治愈感染或减少共价闭合环状 DNA（cccDNA）的数量。HBV 核心蛋白是一种由 183 个氨基酸组成的小蛋白，参与 HBV 复制周期的多种基本功能。正在开发针对核心蛋白的衣壳组装调节剂。磺酰胺是一种合成功能基团，存在于几种药物中。本文简要介绍了磺酰胺苯甲酰胺作为 HBV 衣壳调节剂的情况，并介绍了在其设计和开发中使用的药物化学策略。
