ArticlePloS one2019
Discovery of novel West Nile Virus protease inhibitor based on isobenzonafuranone and triazolic derivatives of eugenol and indan-1,3-dione scaffolds.
Article in PloS one, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 28 citations in OpenAlex.
- Surveillance of the antiviral activity and mechanism of action of newly synthesized spirocyclic thio-pyrimidinones against human adenovirus type 40.Virology journal · 2026Article
- West Nile Virus: Epidemiology, Surveillance, and Prophylaxis with a Comparative Insight from Italy and Iran.Vaccines · 2026Review
- A novel approach utilizing spirocyclic thiopyrimidinone compounds against herpes simplex virus with underlying antiviral mechanisms of action.Virology journal · 2025Article
- West Nile virus - a re-emerging global threat: recent advances in vaccines and drug discovery.Frontiers in cellular and infection microbiology · 2025Review
- Design and Synthesis of Eugenol Derivatives Bearing a 1,2,3-Triazole Moiety for Papaya Protection againstJournal of agricultural and food chemistry · 2024Article
- From clove oil to bioactive agents: synthetic routes, antimicrobial and antiparasitic activities of eugenol derivatives.Future medicinal chemistry · 2024Review
- Synthesis of 1,2,3-Triazole-Containing Methoxylated Cinnamides and Their Antileishmanial Activity against thePharmaceuticals (Basel, Switzerland) · 2023Article
- In Vitro Antiviral Potential, Antioxidant, and Chemical Composition of Clove (Molecules (Basel, Switzerland) · 2023Article
- Clove Essential Oil (Molecules (Basel, Switzerland) · 2021Review
- Review
- Targeting the protease of West Nile virus.RSC medicinal chemistry · 2021Review
- Screening of phytoconstituents of Andrographis paniculata against various targets of Japanese encephalitis virus: An in-silico and in-vitro target-based approach.Current research in pharmacology and drug discovery · 2021Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The West Nile Virus (WNV) NS2B-NS3 protease is an attractive target for the development of therapeutics against this arboviral pathogen. In the present investigation, the screening of a small library of fifty-eight synthetic compounds against the NS2-NB3 protease of WNV is described. The following groups of compounds were evaluated: 3-(2-aryl-2-oxoethyl)isobenzofuran-1(3H)-ones; eugenol derivatives bearing 1,2,3-triazolic functionalities; and indan-1,3-diones with 1,2,3-triazolic functionalities. The most promising of these was a eugenol derivative, namely 4-(3-(4-allyl-2-methoxyphenoxy)-propyl)-1-(2-bromobenzyl)-1H-1,2,3-triazole (35), which inhibited the protease with IC50 of 6.86 μmol L-1. Enzyme kinetic assays showed that this derivative of eugenol presents competitive inhibition behaviour. Molecular docking calculations predicted a recognition pattern involving the residues His51 and Ser135, which are members of the catalytic triad of the WNV NS2B-NS3 protease.
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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.