Publications by authors named "V I Uvarova"
Article Synopsis
- X-ray structures of coronavirus drug targets were rapidly acquired during the early COVID-19 pandemic, especially focusing on the main protease (Mpro) of SARS-CoV-2, which is crucial for developing direct antiviral drugs.
- A systematic, semi-automated method was developed to select the best ensemble of Mpro structures for virtual screening of potential inhibitors, as the selection process was complex.
- This method was validated against existing approaches and led to the discovery of new thienopyrimidinone derivatives that effectively inhibit the Mpro enzyme.
Article Synopsis
- The addition of lipophilic groups to nucleoside analogues enhances their antiviral potency, particularly against viruses like TBEV and EV-A71.
- Researchers synthesized a series of N-benzyladenosine analogues using specific cross-coupling methods to analyze their effectiveness against different flaviviruses and enteroviruses.
- The compounds showed strong inhibition of flavivirus replication at low concentrations, targeting viral RNA synthesis while displaying minimal cytotoxicity, but they did not affect enterovirus reproduction, suggesting a unique mechanism focused on flaviviruses.
3-[-Bis(sulfonyl)amino]isoxazolines with Spiro-Annulated or 1,2-Annulated Cyclooctane Rings Inhibit Reproduction of Tick-Borne Encephalitis, Yellow Fever, and West Nile Viruses.
Int J Mol Sci
June 2023
Spirocyclic compounds containing heterocyclic moieties represent promising 3D scaffolds for modern drug design. In the search for novel anti-flaviviral agents, we have obtained a series of 3-[-bis(sulfonyl)amino]isoxazolines containing spiro-annulated cyclooctane rings and assessed their antiviral activity against tick-borne encephalitis (TBEV), yellow fever (YFV), and West Nile (WNV) viruses. The structural analogs of spirocyclic compounds with a single sulfonyl group or 1,2-annulated cyclooctane ring were also investigated.
View Article and Find Full Text PDFTick-borne encephalitis virus (TBEV), yellow fever virus (YFV), and West Nile virus (WNV) are flaviviruses causing emerging arthropod-borne infections of a great public health concern. Clinically approved drugs are not available to complement or replace the existing vaccines, which do not provide sufficient coverage. Thus, the discovery and characterization of new antiflaviviral chemotypes would advance studies in this field.
View Article and Find Full Text PDFAmphipathic nucleoside and non-nucleoside derivatives of pentacyclic aromatic hydrocarbon perylene are known as potent non-cytotoxic broad-spectrum antivirals. Here we report 3-methyl-5-(perylen-3-ylethynyl)-uracil-1-acetic acid and its amides, a new series of compounds based on a 5-(perylen-3-ylethynyl)-uracil scaffold. The compounds demonstrate pronounced in vitro activity against arthropod-borne viruses, namely tick-borne encephalitis virus (TBEV) and yellow fever virus (YFV), in plaque reduction assays with EC values below 1.
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