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Pharmacologic background and clinical issue of anti-influenza drugs.
Fukushima J Med Sci
December 2024
Department of Pediatrics, Fukushima Medical University.
Since 2000, rapid antigen detection kits and anti-influenza drugs have been used for the early diagnosis and treatment of influenza in Japan, respectively. The main drugs available in clinical practice are the neuraminidase inhibitors oseltamivir, zanamivir, laninamivir, and peramivir, as well as the cap-dependent endonuclease inhibitor baloxavir marboxil. Antiviral therapy with neuraminidase inhibitors has been practiced for many years, especially in Japan; it can shorten the febrile period and reduce complications.
View Article and Find Full Text PDFAntiviral Activity of (1,9a)-1-[(1,2,3-Triazol-1-yl)methyl]octahydro-1-quinolizines from the Alkaloid Lupinine.
Molecules
December 2024
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 630090 Novosibirsk, Russia.
Influenza is a disease of significant morbidity and mortality. The number of anti-influenza drugs is small; many of them stimulate the appearance of resistant strains. This article presents the results of assessing the antiviral activity of 1,2,3-triazole-containing derivatives of alkaloid lupinine for their ability to suppress the reproduction of orthomyxoviruses (influenza viruses: A/Vladivostok/2/09 (H1N1) and A/Almaty/8/98 (H3N2)).
View Article and Find Full Text PDFMolecular dynamics study on the effect of the N1 neuraminidase double mutant G147R/H274Y on oseltamivir sensitivity.
RSC Adv
December 2024
Bioinformatics Research Group, University-CoE-Research Center for Bio-Molecule Engineering (BIOME), Universitas Airlangga Surabaya 60115 Indonesia.
Inhibition of neuraminidase is the most prominent target in influenza medication using oseltamivir as an inhibitor. However, the emerging resistance of neuraminidase toward oseltamivir due to mutation reduces the efficacy of oseltamivir. The generally reported mutation is a single mutation at H274Y, which declines the sensitivity of oseltamivir by almost 900 folds compared to the wild-type variant.
View Article and Find Full Text PDFDiscovery of Novel Thiophene-Based Baloxavir Derivatives as Potent Cap-Dependent Endonuclease Inhibitors for Influenza Treatment.
J Med Chem
December 2024
Shenzhen Key Laboratory of Small Molecule Drug Discovery and Synthesis, Department of Chemistry, Shenzhen Grubbs Institute and Medi-X Pingshan, Southern University of Science and Technology, Shenzhen 518000, China.
The genetic recombination and antigenic variation of influenza viruses may decrease the efficacy of antiviral vaccines, highlighting the imperativeness of developing novel anti-influenza agents. Herein, a series of thiophene-based compounds were designed and synthesized as potent anti-influenza agents. Among them, exhibited an excellent anti-influenza activity (EC, H1N1 = 1.
View Article and Find Full Text PDFDevelopment of Broad-Spectrum β-Cyclodextrins-Based Nanomaterials Against Influenza Viruses.
J Med Virol
December 2024
Department of Microbiology and Molecular Medicine, University of Geneva, Geneva, Switzerland.
In recent decades, epidemics and pandemics have multiplied throughout the world, with viruses generally being the primary responsible agents. Among these, influenza viruses play a key role, as they potentially cause severe respiratory distress, representing a major threat to public health. Our study aims to develop new broad-spectrum antivirals against influenza to improve the response to viral disease outbreaks.
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