{
  "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 EC₅₀ values in the low nanomolar range and minimal cytotoxicity. This work broadens the chemical space surrounding GLP-26 and provides a valuable roadmap for designing new scaffolds for next-generation HBV CAMs.",
  "abstract_shown": true,
  "affiliations": [
    "Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, Atlanta, GA 30322, USA. rschina@emory.edu."
  ],
  "article_type": "research article",
  "arxiv": null,
  "author_total": 15,
  "authors": [
    {
      "affs": [
        0
      ],
      "name": "Zhe Chen"
    },
    {
      "affs": [
        0
      ],
      "name": "Shaoman Zhou"
    },
    {
      "affs": [
        0
      ],
      "name": "Peng Liu"
    },
    {
      "affs": [
        0
      ],
      "name": "John Wiseman"
    },
    {
      "affs": [
        0
      ],
      "name": "Longhu Zhou"
    },
    {
      "affs": [
        0
      ],
      "name": "Chia-Han Vanessa Fan"
    },
    {
      "affs": [
        0
      ],
      "name": "Heather B Bowers",
      "orcid": "0000-0001-8758-8633"
    },
    {
      "affs": [
        0
      ],
      "name": "Mohammad Salman"
    },
    {
      "affs": [
        0
      ],
      "name": "Kiran Verma"
    },
    {
      "affs": [
        0
      ],
      "name": "Danielle R Monroe"
    },
    {
      "affs": [
        0
      ],
      "name": "Jessica Downs-Bowen"
    },
    {
      "affs": [
        0
      ],
      "name": "Dharmeshkumar Patel",
      "orcid": "0000-0003-1601-256X"
    },
    {
      "affs": [
        0
      ],
      "name": "Leda Bassit"
    },
    {
      "affs": [
        0
      ],
      "name": "Raymond F Schinazi"
    },
    {
      "affs": [
        0
      ],
      "name": "Franck Amblard",
      "orcid": "0009-0002-6235-4050"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/254ettzem0n0m.bib",
  "cited_by": 0,
  "doi": "10.1039/d6ob00943c",
  "fulltext_url": "https://europepmc.org/articles/PMC13650461",
  "id": "254ettzem0n0m",
  "issns": [
    "1477-0520",
    "1477-0539"
  ],
  "landing_url": "https://europepmc.org/article/MED/42851025",
  "language": "eng",
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "openalex",
      "2713|Hepatitis B Virus Studies"
    ]
  ],
  "openalex": "W7220436538",
  "pdf_url": "https://pubs.rsc.org/ob/article-pdf/doi/10.1039/D6OB00943C/14825808/d6ob00943c.pdf",
  "pmcid": "PMC13650461",
  "pmid": "42851025",
  "published": "2026-10-21",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/254ettzem0n0m.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:18:02Z",
      "native_id": "MED:42851025",
      "source": "europepmc",
      "url": "https://europepmc.org/article/MED/42851025"
    }
  ],
  "subjects": [
    {
      "field": "medicine",
      "origin": "openalex:2713|Hepatitis B Virus Studies",
      "subfield": "epidemiology-public-health"
    }
  ],
  "title": "4-Diketopyrrole-2-carboxamide derivatives affecting HBV capsid assembly: structure-activity relationship around the GLP-26 scaffold.",
  "title_text": "4-Diketopyrrole-2-carboxamide derivatives affecting HBV capsid assembly: structure-activity relationship around the GLP-26 scaffold.",
  "type": "peer-reviewed",
  "updated_at": "2026-10-30T12:18:02Z",
  "url": "https://research.draconitic.com/paper/254ettzem0n0m",
  "venue": "Organic & biomolecular chemistry",
  "versions": []
}