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- Title
Bioactive Pyrrolo[2,1- f ][1,2,4]triazines: Synthesis, Molecular Docking, In Vitro Cytotoxicity Assay and Antiviral Studies.
- Authors
Mochulskaya, Nataliya N.; Kotovskaya, Svetlana K.; Butorin, Ilya I.; Varaksin, Mikhail V.; Charushin, Valery N.; Rusinov, Vladimir L.; Esaulkova, Yana L.; Slita, Alexander V.; Ilyina, Polina A.; Zarubaev, Vladimir V.
- Abstract
A series of 2,4-disubstituted pyrrolo[2,1-f][1,2,4]triazines containing both aryl and thienyl substituents were synthesized by exploiting the 1,3-cycloaddition reaction of N(1)-ethyl-1,2,4-triazinium tetrafluoroborates with dimethyl acetylenedicarboxylate. The antiviral activity of the synthesized compounds against influenza virus strain A/Puerto Rico/8/34 (H1N1) was studied in experiments on Madin-Darby canine kidney (MDCK) cell culture. Among the pyrrolo[2,1-f][1,2,4]triazine derivatives, compounds with low toxicity and high antiviral activity were identified. Dimethyl 4-(4-methoxyphenyl)-7-methyl-2-p-tolylpyrrolo[2,1-f][1,2,4]triazine-5,6-dicarboxylate was found to demonstrate the best antiviral activity (IC50 4 µg/mL and selectivity index 188). Based on the results of in vitro tests and molecular docking studies performed, a plausible mechanism of action for these compounds was suggested to involve inhibition of neuraminidase.
- Subjects
PUERTO Rico; NEURAMINIDASE; MOLECULAR docking; CYTOTOXINS; TRIAZINE derivatives; TRIAZINES; CHEMICAL synthesis; TETRAFLUOROBORATES; INFLUENZA viruses
- Publication
Chemistry (2624-8549), 2023, Vol 5, Issue 4, p2657
- ISSN
2624-8549
- Publication type
Article
- DOI
10.3390/chemistry5040171