ArticleOrganic & biomolecular chemistry2026
4-Diketopyrrole-2-carboxamide derivatives affecting HBV capsid assembly: structure-activity relationship around the GLP-26 scaffold.
Article in Organic & biomolecular chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
15 authors.
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Abstract
Chronic hepatitis B virus (HBV) infection remains a major global health burden with limited curative options. Capsid assembly modulators (CAMs) have emerged as a promising antiviral strategy by disrupting nucleocapsid formation and suppressing cccDNA amplification. In this study, we discuss the structure-activity relationship (SAR) around the 4-diketopyrrole-2-carboxamide scaffold of GLP-26, focusing on modifying the aniline moiety and the oxoacetamide region, and introducing alternative acetamide groups. Compounds were synthesized through efficient coupling strategies, including microwave-assisted amidation, and several analogs exhibited potent inhibition of HBV DNA replication in HepAD38 cells, with EC
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Registered trials
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