Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.
Basic Information
ID: ALA4334551
Journal: ACS Med Chem Lett
Title: Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.
Authors: Na HG, Imran A, Kim K, Han HS, Lee YJ, Kim MJ, Yun CS, Jung YS, Lee JY, Han SB.
Abstract: 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.
CiteXplore: 32071684
DOI: 10.1021/acsmedchemlett.9b00550
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