Design, synthesis and antiviral evaluation of triazole-linked 7-hydroxycoumarin-monoterpene conjugates as inhibitors of RSV replication
RSC Medicinal Chemistry, ISSN: 2632-8682
2024
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Investigators from N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry Zero in on Respiratory Syncytial Viruses (Design, Synthesis and Antiviral Evaluation of Triazole-linked 7-hydroxycoumarin-monoterpene Conjugates As Inhibitors of Rsv ...)
2025 JAN 23 (NewsRx) -- By a News Reporter-Staff News Editor at NewsRx Drug Daily -- Fresh data on RNA Viruses - Respiratory Syncytial Viruses
Article Description
Respiratory syncytial virus (RSV) is the leading cause of acute lower respiratory infections in babies across the world. Irrespective of progress in the development of RSV vaccines, effective small molecule drugs are still not available on the market. Based on our previous data we designed and synthesized triazole-linked coumarin-monoterpene hybrids and showed that they are indeed effective in inhibiting the RSV replication. The most effective compounds are active against both RSV serotypes, A and B, with IC in the low micromolar or submicromolar range of concentrations. These are the most active coumarin derivatives found so far. Compound 45 combining 3,7-dimethyloctane and cyclopentane-annealed coumarin fragments has a selectivity index of 160 for serotype A and 1147 for serotype B. According to the results of the time-of-addition experiments, the conjugates are active at the early stages of the virus cycle. Based on biological evaluation and molecular modeling data, RSV F protein is a possible target.
Bibliographic Details
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85214142480&origin=inward; http://dx.doi.org/10.1039/d4md00728j; http://www.ncbi.nlm.nih.gov/pubmed/39760101; https://xlink.rsc.org/?DOI=D4MD00728J; https://dx.doi.org/10.1039/d4md00728j; https://pubs.rsc.org/en/content/articlelanding/2025/md/d4md00728j
Royal Society of Chemistry (RSC)
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