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Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.


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.

SUBMITTER: Na HG 

PROVIDER: S-EPMC7025384 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.

Na Hyo Gyeong HG   Imran Ali A   Kim Kyuneun K   Han Hong Sik HS   Lee Young Jin YJ   Kim Myung-Jin MJ   Yun Chang-Soo CS   Jung Young-Sik YS   Lee Joo-Youn JY   Han Soo Bong SB  

ACS medicinal chemistry letters 20200109 2


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 vi  ...[more]

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