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Discovery and optimization of benzenesulfonamides-based hepatitis B virus capsid modulators via contemporary medicinal chemistry strategies.

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Ren Y,Ma Y,Cherukupalli S,Tavis JE,Menéndez-Arias L,Liu X,Zhan P

doi

10.1016/j.ejmech.2020.112714

subject

Has Abstract

pub_date

2020-11-15 00:00:00

pages

112714

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30686-3

journal_volume

206

pub_type

杂志文章,评审

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