ArticleJournal of medicinal chemistry2015
5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- Recent advances in triazole hybrid molecules for the therapeutic management of neglected tropical diseases.RSC medicinal chemistry · 2025Review
- Advances in antiviral strategies targeting mosquito-borne viruses: cellular, viral, and immune-related approaches.Virology journal · 2025Review
- The role of silicon in drug discovery: a review.RSC medicinal chemistry · 2024Review
- Dengue virus: pathogenesis and potential for small molecule inhibitors.Bioscience reports · 2024Review
- The endoplasmic reticulum (ER): a crucial cellular hub in flavivirus infection and potential target site for antiviral interventions.Npj viruses · 2024Review
- Review
- Development in the Inhibition of Dengue Proteases as Drug Targets.Current medicinal chemistry · 2024Review
- Development of a luminescence-based method for measuring West Nile Virus MTase activity and its application to screen for antivirals.Current research in microbial sciences · 2024Article
- Recent Progress on Synthesis of Functionalized 1,5-Disubstituted Triazoles.Current organic synthesis · 2024Review
- Nucleoside Analog 2',3'-Isopropylidene-5-Iodouridine as Novel Efficient Inhibitor of HIV-1.Pharmaceutics · 2023Article
- Review
- Antiviral effects of the fused tricyclic derivatives of indoline and imidazolidinone on ZIKV infection and RdRp activities of ZIKV and DENV.Virus research · 2023Article
- The Use of Zidovudine Pharmacophore in Multi-Target-Directed Ligands for AIDS Therapy.Molecules (Basel, Switzerland) · 2022Review
- Seeking heterocyclic scaffolds as antivirals against dengue virus.European journal of medicinal chemistry · 2022Review
- Review
- Chemical biology and medicinal chemistry of RNA methyltransferases.Nucleic acids research · 2022Article
- Updates on Dengue Vaccine and Antiviral: Where Are We Heading?Molecules (Basel, Switzerland) · 2021Review
- Development of Triazoles and Triazolium Salts Based on AZT and Their Anti-Viral Activity against HIV-1.Molecules (Basel, Switzerland) · 2021Article
- Broad-Spectrum Antiviral Activity of 3'-Deoxy-3'-Fluoroadenosine against Emerging Flaviviruses.Antimicrobial agents and chemotherapy · 2021Article
- Antiviral and Antimicrobial Nucleoside Derivatives: Structural Features and Mechanisms of Action.Molecular biology · 2021Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
West Nile virus (WNV) and Dengue virus (DENV) are important human pathogens for which there are presently no vaccine or specific antivirals. We report herein a 5'-silylated nucleoside scaffold derived from 3'-azidothymidine (AZT) consistently and selectively inhibiting WNV and DENV at low micromolar concentrations. Further synthesis of various triazole bioisosteres demonstrated clear structure-activity relationships (SARs) in which the antiviral activity against WNV and DENV hinges largely on both the 5'-silyl group and the substituent of 3'-triazole or its bioisosteres. Particularly interesting is the 5' silyl group which turns on the antiviral activity against WNV and DENV while abrogating the previously reported antiviral potency against human immunodeficiency virus (HIV-1). The antiviral activity was confirmed through a plaque assay where viral titer reduction was observed in the presence of selected compounds. Molecular modeling and competitive S-adenosyl-l-methionine (SAM) binding assay suggest that these compounds likely confer antiviral activity via binding to methyltransferase (MTase).
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