{
  "abstract": "Screening of the open-access CRESTdb small-molecule library identified the imidazothiazole carboxamide sCQG200 (1) as an initial hit, with activity against H37Rv and Erdman Mycobacterium tuberculosis strains in cholesterol-containing medium (MIC90= 6.88 uM and 4.48 uM, respectively) and against intracellular Mtb (EC50= 3.80 uM). sCQG200 retained activity against drug-resistant Mtb strains, including clinical MDR/XDR isolates. SAR optimization led to analogs 21 and 24 with substantially improved antimycobacterial potency. Mouse pharmacokinetic studies following oral and intravenous administration showed 62.1% and 29.5% oral bioavailability for 21 and 24, respectively. This structurally differentiated chemotype provides a promising starting point for further optimization as antitubercular agent.",
  "abstract_shown": true,
  "affiliations": [
    "Calibr-Skaggs Institute for Innovative Medicines, a division of Scripps Research"
  ],
  "article_type": "New results",
  "arxiv": null,
  "author_total": 9,
  "authors": [
    {
      "name": "L. Meng"
    },
    {
      "name": "D. Grant"
    },
    {
      "name": "H. Xie"
    },
    {
      "name": "R. Ford"
    },
    {
      "name": "J. Webb"
    },
    {
      "name": "C. W. McNamara"
    },
    {
      "name": "P. Sukheja"
    },
    {
      "affs": [
        0
      ],
      "name": "B. Yang"
    },
    {
      "name": "A. K. Chatterjee"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/c7zcvd6q1ccmp.bib",
  "cited_by": 0,
  "doi": "10.64898/2026.09.21.753226",
  "fulltext_url": "https://www.biorxiv.org/content/10.64898/2026.09.21.753226v1.full",
  "id": "c7zcvd6q1ccmp",
  "issns": [],
  "landing_url": "https://www.biorxiv.org/content/10.64898/2026.09.21.753226v1",
  "language": null,
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "biorxiv",
      "microbiology"
    ],
    [
      "openalex",
      "2725|Tuberculosis Research and Epidemiology"
    ]
  ],
  "openalex": "W7214197786",
  "pdf_url": "https://www.biorxiv.org/content/10.64898/2026.09.21.753226v1.full.pdf",
  "pmcid": null,
  "pmid": null,
  "published": "2026-09-21",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/c7zcvd6q1ccmp.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:24:19Z",
      "native_id": "10.64898/2026.09.21.753226",
      "source": "biorxiv",
      "url": "https://www.biorxiv.org/content/10.64898/2026.09.21.753226v1"
    }
  ],
  "subjects": [
    {
      "field": "biology",
      "origin": "biorxiv:microbiology",
      "subfield": "microbiology"
    }
  ],
  "title": "Discovery and Optimization of Imidazothiazole Carboxamides as Novel Anti-Tuberculosis Agents",
  "title_text": "Discovery and Optimization of Imidazothiazole Carboxamides as Novel Anti-Tuberculosis Agents",
  "type": "preprint",
  "updated_at": "2026-10-30T12:24:19Z",
  "url": "https://research.draconitic.com/paper/c7zcvd6q1ccmp",
  "venue": "bioRxiv",
  "versions": []
}