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primary topic: Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2

Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2
type: AcademicArticle
type: Article
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.
date: 2026-04-13
volume: 69
issue: 8
status: peerReviewed
status: published
author list: authors
type: EPrint
type: ArticleEPrint
is part of: repository
has document: Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2 (HTML)
subject: QR Microbiology

Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2 (HTML)
type: Document
has file: references (6).bib
has part: references (6).bib

AMER CHEMICAL SOC
type: Organization

JOURNAL OF MEDICINAL CHEMISTRY
type: Collection

Vinod D. Chaudhari
type: Person
given name: Vinod D.
family name: Chaudhari

Simran Kaur
type: Person
given name: Simran
family name: Kaur

Nittu Singh
type: Person
given name: Nittu
family name: Singh

Sumit Dhiman
type: Person
given name: Sumit
family name: Dhiman

Deshkanwar S. Brar
type: Person
given name: Deshkanwar S.
family name: Brar

Utpal Nandi
type: Person
given name: Utpal
family name: Nandi

Ravneet S. Chawla
type: Person
given name: Ravneet S.
family name: Chawla

Rajesh P. Ringe
type: Person
given name: Rajesh P.
family name: Ringe

Sahil Kumar
type: Person
given name: Sahil
family name: Kumar

Krishan G. Thakur
type: Person
given name: Krishan G.
family name: Thakur

Akshay Joshi
type: Person
given name: Akshay
family name: Joshi

HTML Summary of #3458 Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2
format: text/html
primary topic: Development of Benzimidazole-Based BZ-30 as an Orally Bioavailable Broad-Spectrum Inhibitor of SARS-CoV-2

QR Microbiology
type: Concept