Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.,ACS Medicinal Chemistry Letters

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Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-09 , DOI: 10.1021/acsmedchemlett.9b00550
Hyo Gyeong Na _{1,

2} , Ali Imran ₁ , Kyuneun Kim _{1,

2} , Hong Sik Han _{1,

2} , Young Jin Lee _{1,

2} , Myung-Jin Kim ₃ , Chang-Soo Yun ₁ , Young-Sik Jung _{1,

2} , Joo-Youn Lee ₄ , Soo Bong Han _{1,

2}

Affiliation

Hepatitis B virus (HBV) remains a major health concern with 260 million people having been infected globally, and approximately 680,000 deaths have occurred annually from cirrhosis and liver cancer. The modulation of HBV capsid assembly has emerged as a promising therapeutic approach for curing chronic HBV infection. Small-molecule capsid assembly modulators (CAMs) can broadly be classified as heteroaryldihydropyrimidines and sulfamoylbenzamides (SBAs). SBAs are capsid activators that inhibit viral replication by achieving capsid assembly before polymerase encapsulation. Herein, we report a novel series of HBV CAMs based on NVR 3-778, a potent CAM belonging to the SBA class. The lead compound (KR-26556) exhibited improved pharmacological activity and was examined through molecular docking studies.

中文翻译：

发现一种新的磺酰胺乙型肝炎衣壳组装调节剂。

乙型肝炎病毒 (HBV) 仍然是一个主要的健康问题，全球有 2.6 亿人被感染，每年约有 68 万人死于肝硬化和肝癌。HBV 衣壳组装的调节已成为治疗慢性 HBV 感染的一种有前途的治疗方法。小分子衣壳组装调节剂（CAM）大致可分为杂芳基二氢嘧啶和氨磺酰苯甲酰胺（SBA）。SBA 是衣壳激活剂，通过在聚合酶封装之前实现衣壳组装来抑制病毒复制。在此，我们报告了一系列基于 NVR 3-778 的新型 HBV CAM，这是一种属于 SBA 类的有效 CAM。先导化合物 (KR-26556) 表现出改善的药理活性，并通过分子对接研究进行了检查。

更新日期：2020-01-15

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