@ARTICLE{Kaur2026-xt,
  title     = "Development of benzimidazole-based {BZ-30} as an orally
               bioavailable broad-spectrum inhibitor of {SARS-CoV-2}",
  author    = "Kaur, Simran and Brar, Deshkanwar S and Joshi, Akshay and Singh,
               Nittu and Chawla, Ravneet S and Kumar, Sahil and Dhiman, Sumit
               and Nandi, Utpal and Ringe, Rajesh P and Thakur, Krishan G and
               Chaudhari, Vinod D",
  abstract  = "Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2),
               the etiological agent of the 2019 global pandemic, continues to
               undermine therapeutic interventions due to its high
               transmissibility and mutability. This highlights the need for
               potent antivirals capable of combating emerging variants and
               controlling outbreaks. Here, we report the discovery and
               development of the first-in-class novel benzimidazole (BZ)
               derivatives as potent inhibitors of SARS-CoV-2. Through
               antiviral screening, the benzimidazolone derivative (I) was
               found as the hit. Further hit-to-lead optimization led to BZ
               compounds with submicromolar IC50 values. Mechanistically, these
               compounds partially inhibit endocytosis entry pathways. The
               compounds shortlisted have broad-spectrum antiviral profiles
               against different variants of concern. Notably, BZ-01 and BZ-30
               show good pharmacokinetic properties, with BZ-30 displaying
               excellent oral bioavailability. Evaluation of BZ-30 in
               SARS-CoV-2-challenged hamsters significantly reduced viral load
               and improved lung pathology, indicating its in vivo antiviral
               efficacy and highlighting its therapeutic potential as an orally
               available antiviral candidate.",
  journal   = "J. Med. Chem.",
  publisher = "American Chemical Society (ACS)",
  volume    =  69,
  number    =  8,
  pages     = "9537--9557",
  month     =  apr,
  year      =  2026,
  language  = "en"
}