Zika virus (ZIKV) is a mosquito-transmitted Flavivirus, originally identified in Uganda in 1947 and recently associated with a large outbreak in South America. Despite extensive efforts there are currently no approved antiviral compounds for treatment of ZIKV infection. Here we describe the antiviral activity of diarylamines derived from anthranilic acid (FAMs) against ZIKV. A synthetic FAM (E3) demonstrated anti-ZIKV potential by reducing viral replication up to 86%. We analyzed the possible mechanisms of action of FAM E3 by evaluating the intercalation of this compound into the viral dsRNA and its interaction with the RNA polymerase of bacteriophage SP6. However, FAM E3 did not act by these mechanisms. In silico results predicted that FAM E3 might bind to the ZIKV NS3 helicase suggesting that this protein could be one possible target of this compound. To test this, the thermal stability and the ATPase activity of the ZIKV NS3 helicase domain (NS3) were investigated in vitro and we demonstrated that FAM E3 could indeed bind to and stabilize NS3.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6881388 | PMC |
| http://dx.doi.org/10.1038/s41598-019-54169-z | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Targeting Lung Cancer with Carvacrol-Triazole-Arylidenehydrazide Hybrids: In Vitro and In Silico Cytotoxicity Assessments.
Chem Biodivers
January 2025
Bezmialem Vakif University: Bezmialem Vakif Universitesi, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Vatan St., 34093, Istanbul, TURKEY.
In this study, a series of 16 arylidenehydrazide derivatives (7a-7p), hybridized with the natural product carvacrol, were successfully synthesized starting from anthranilic acid methyl ester. The cytotoxic effects of these compounds were examined against two different cell lines, A549 and BEAS-2B. Additionally, in silico studies were conducted to investigate the ligand-protein binding modes and their stabilities.
View Article and Find Full Text PDFGreen one-pot synthesis of quinoxaline derivatives using sulfo-anthranilic acid functionalized alginate-MCFeO nanostructures: a novel superparamagnetic catalyst with antiproliferative potential.
RSC Adv
January 2025
Department of Life Science and Agriculture, Zhoukou Normal University Zhoukou Henan 466001 China
This study reports a green, multi-component synthesis of 2-aminoimidazole-linked quinoxaline Schiff bases using a novel superparamagnetic acid catalyst. The catalyst consists of sulfo-anthranilic acid (SAA) immobilized on MnCoFeO@alginate magnetic nanorods (MNRs), achieving high SAA loading (1.8 mmol g) and product yields (91-97%).
View Article and Find Full Text PDFIdentification of a binding site for small molecule inhibitors targeting human TRPM4.
Nat Commun
January 2025
Laboratory of Biological Electron Microscopy, IPHYS, SB, EPFL, and Dept. Fundamental Microbiology, Faculty of Biology and Medicine, UNIL, Cubotron, Rt. de la Sorge, Lausanne, Switzerland.
Transient receptor potential (TRP) melastatin 4 (TRPM4) protein is a calcium-activated monovalent cation channel associated with various genetic and cardiovascular disorders. The anthranilic acid derivative NBA is a potent and specific TRPM4 inhibitor, but its binding site in TRPM4 has been unknown, although this information is crucial for drug development targeting TRPM4. We determine three cryo-EM structures of full-length human TRPM4 embedded in native lipid nanodiscs without inhibitor, bound to NBA, and an anthranilic acid derivative, IBA.
View Article and Find Full Text PDFManganese(II) Complexes with Non-Steroidal Anti-Inflammatory Drugs: Structure and Biological Activity.
Int J Mol Sci
December 2024
Department of General and Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece.
Nine manganese(II) complexes with a series of non-steroidal anti-inflammatory drugs (namely sodium diclofenac, diflunisal, flufenamic acid, sodium meclofenamate, mefenamic acid, and tolfenamic acid) were prepared in the presence of diverse nitrogen donors, i.e., pyridine, 1,10-phenanthroline, 2,2'-bipyridine and neocuproine, as co-ligands and were characterized with spectroscopic techniques and single-crystal X-ray crystallography.
View Article and Find Full Text PDFCompared Inhibitory Activities of Tamoxifen and Avenanthramide B on Liver Esterase and Correlation Based on the Superimposed Structure Between Porcine and Human Liver Esterase.
Int J Mol Sci
December 2024
Department of Biological Science, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Exposure to tamoxifen can exert effects on the human liver, and esterases process prodrugs such as antibiotics and convert them to less toxic metabolites. In this study, the porcine liver esterase (PLE)-inhibitory activity of tamoxifen has been investigated. PLE showed inhibition of a PLE isoenzyme (PLE5).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!