tetano
Editor, Senior Moderator
Mol Divers. 2018 Jul 3. doi: 10.1007/s11030-018-9840-5. [Epub ahead of print]
[h=1]Structural modification on rupestonic acid leads to highly potent inhibitors against influenza virus.[/h] Obul M[SUP]1,[/SUP][SUP]2[/SUP], Wang X[SUP]1,[/SUP][SUP]2[/SUP], Zhao J[SUP]1[/SUP], Li G[SUP]1[/SUP], Aisa HA[SUP]3[/SUP], Huang G[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza viruses are responsible for seasonal epidemics and occasional pandemics, which cause significant morbidity and mortality. Although several drugs (adamantanes and neuraminidase inhibitors) are available in the market, the worldwide spread of drug-resistant influenza strains poses an urgent need for novel antiviral drugs. Artemisia rupestris L. is a folk medicine used to treat cold. In this paper, we structurally modified rupestonic acid, a bioactive component of A. rupestris, to synthesize a series of 2-substituted rupestonic acid methyl esters (3a-3o). Their structures were fully characterized by [SUP]1[/SUP]H NMR, [SUP]13[/SUP]C NMR, HRMS spectra. Among them, compounds 3b and 3c exhibited potent activities against influenza H1N1 with micromolar IC[SUB]50[/SUB] values and might serve as new lead compounds for the treatment of influenza.
[h=4]KEYWORDS:[/h] Artemisia rupestris; Benzylation; Influenza virus; Rupestonic acid
PMID: 29971616 DOI: 10.1007/s11030-018-9840-5
[h=1]Structural modification on rupestonic acid leads to highly potent inhibitors against influenza virus.[/h] Obul M[SUP]1,[/SUP][SUP]2[/SUP], Wang X[SUP]1,[/SUP][SUP]2[/SUP], Zhao J[SUP]1[/SUP], Li G[SUP]1[/SUP], Aisa HA[SUP]3[/SUP], Huang G[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza viruses are responsible for seasonal epidemics and occasional pandemics, which cause significant morbidity and mortality. Although several drugs (adamantanes and neuraminidase inhibitors) are available in the market, the worldwide spread of drug-resistant influenza strains poses an urgent need for novel antiviral drugs. Artemisia rupestris L. is a folk medicine used to treat cold. In this paper, we structurally modified rupestonic acid, a bioactive component of A. rupestris, to synthesize a series of 2-substituted rupestonic acid methyl esters (3a-3o). Their structures were fully characterized by [SUP]1[/SUP]H NMR, [SUP]13[/SUP]C NMR, HRMS spectra. Among them, compounds 3b and 3c exhibited potent activities against influenza H1N1 with micromolar IC[SUB]50[/SUB] values and might serve as new lead compounds for the treatment of influenza.
[h=4]KEYWORDS:[/h] Artemisia rupestris; Benzylation; Influenza virus; Rupestonic acid
PMID: 29971616 DOI: 10.1007/s11030-018-9840-5