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Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication.


ABSTRACT: As the spread of infections caused by hepatitis B virus (HBV) threatens public health worldwide, investigations from multiple perspectives and of various mechanisms of action are urgently required to increase the HBV cure rate. Targeting the encapsidation of the nuclear capsid protein (core protein, HBc) has emerged as an attractive strategy for inhibiting the viral assembly process; however, a drug targeting this mechanism has not yet been approved. We synthesized novel sulfamoylbenzamides (SBAs) as capsid assembly modulators of HBV and found that the effects and safety profiles of compounds 3 and 8 have potential therapeutic applicability against HBV. The formation of tubular particles was time-dependent in the presence of 3, indicating a new mode of protein assembly by SBA compounds. Our findings provide a new entity for developing safe and efficient treatments for HBV infection.

SUBMITTER: Lee YH 

PROVIDER: S-EPMC7883466 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature

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Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication.

Lee Yeon Hee YH   Cha Hyeon-Min HM   Hwang Jun Yeon JY   Park So Yeong SY   Vishakantegowda Avinash G AG   Imran Ali A   Lee Joo-Youn JY   Yi Yoon-Sun YS   Jun Sangmi S   Kim Ga Hyeon GH   Kang Hyo Jin HJ   Chung Sang J SJ   Kim Meehyein M   Kim Hyejin H   Han Soo Bong SB  

ACS medicinal chemistry letters 20210202 2


As the spread of infections caused by hepatitis B virus (HBV) threatens public health worldwide, investigations from multiple perspectives and of various mechanisms of action are urgently required to increase the HBV cure rate. Targeting the encapsidation of the nuclear capsid protein (core protein, HBc) has emerged as an attractive strategy for inhibiting the viral assembly process; however, a drug targeting this mechanism has not yet been approved. We synthesized novel sulfamoylbenzamides (SBA  ...[more]

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