ArticleBioorganic & medicinal chemistry2008
Heteroaromatic ester inhibitors of hepatitis A virus 3C proteinase: Evaluation of mode of action.
Article in Bioorganic & medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
9 citing papers in PubMed, 22 citations in OpenAlex.
- Targeting the 3C Protease of Hepatitis A Virus Subgenotype IB: Virtual Screening and Identification of Potent Lead Candidates.Microorganisms · 2026Article
- Identification of Mulberrofuran as a potent inhibitor of hepatitis A virus 3CMolecular diversity · 2024Article
- Targeting the Main Protease of SARS-CoV-2: From the Establishment of High Throughput Screening to the Design of Tailored Inhibitors.Angewandte Chemie (International ed. in English) · 2021Article
- Toward development of generic inhibitors against the 3C proteases of picornaviruses.The FEBS journal · 2019Article
- Direct-acting Antivirals and Host-targeting Agents against the Hepatitis A Virus.Journal of clinical and translational hepatology · 2015Review
- Benzotriazole: An overview on its versatile biological behavior.European journal of medicinal chemistry · 2015Review
- Molecular biology and inhibitors of hepatitis A virus.Medicinal research reviews · 2014Review
- Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors.Bioorganic & medicinal chemistry letters · 2009Article
- Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors.Bioorganic & medicinal chemistry letters · 2008Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The related 3C and 3C-like proteinase (3C(pro) and 3CL(pro)) of picornaviruses and coronaviruses, respectively, are good drug targets. As part of an effort to generate broad-spectrum inhibitors of these enzymes, we screened a library of inhibitors based on a halopyridinyl ester from a previous study of the severe acute respiratory syndrome (SARS) 3CL proteinase against Hepatitis A virus (HAV) 3C(pro). Three of the compounds, which also had furan rings, inhibited the cleavage activity of HAV 3C(pro) with K(ic)s of 120-240nM. HPLC-based assays revealed that the inhibitors were slowly hydrolyzed by both HAV 3C(pro) and SARS 3CL(pro), confirming the identity of the expected products. Mass spectrometric analyses indicated that this hydrolysis proceeded via an acyl-enzyme intermediate. Modeling studies indicated that the halopyridinyl moiety of the inhibitor fits tightly into the S1-binding pocket, consistent with the lack of tolerance of the inhibitors to modification in this portion of the molecule. These compounds are among the most potent non-peptidic inhibitors reported to date against a 3C(pro).
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.