tetano
Editor, Senior Moderator
Eur J Med Chem. 2017 Feb 21;130:308-319. doi: 10.1016/j.ejmech.2017.02.028. [Epub ahead of print]
[h=1]Design, synthesis and biological evaluation of gentiopicroside derivatives as potential antiviral inhibitors.[/h] Wu S[SUP]1[/SUP], Yang L[SUP]2[/SUP], Sun W[SUP]2[/SUP], Si L[SUP]3[/SUP], Xiao S[SUP]3[/SUP], Wang Q[SUP]3[/SUP], Dechoux L[SUP]4[/SUP], Thorimbert S[SUP]4[/SUP], Sollogoub M[SUP]4[/SUP], Zhou D[SUP]3[/SUP], Zhang Y[SUP]5[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Based on classical drug design theory, a novel series of gentiopicroside derivatives was designed and synthesized. All synthesized compounds were then biologically evaluated for their inhibition of influenza virus and anti-HCV activity in vitro. Some of the gentiopicroside derivatives, such as 11a, 13d and 16 showed interesting anti-influenza virus activity with IC[SUB]50[/SUB] at 39.5 μM, 45.2 μM and 44.0 μM, respectively. However, no significant anti-HCV activity was found for all of gentiopicroside derivatives. The preliminary results indicate that modification of the sugar moiety on gentiopicroside was helpful for enhancing the anti-influenza activities. Our works demonstrate the importance of secoiridoid natural products as new leads in the development of potential antiviral inhibitors.
Copyright ? 2017 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Antiviral agents; Gentiopicroside derivatives; Natural product; Secoiridoid
PMID: 28254701 DOI: 10.1016/j.ejmech.2017.02.028
[PubMed - as supplied by publisher]
[h=1]Design, synthesis and biological evaluation of gentiopicroside derivatives as potential antiviral inhibitors.[/h] Wu S[SUP]1[/SUP], Yang L[SUP]2[/SUP], Sun W[SUP]2[/SUP], Si L[SUP]3[/SUP], Xiao S[SUP]3[/SUP], Wang Q[SUP]3[/SUP], Dechoux L[SUP]4[/SUP], Thorimbert S[SUP]4[/SUP], Sollogoub M[SUP]4[/SUP], Zhou D[SUP]3[/SUP], Zhang Y[SUP]5[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Based on classical drug design theory, a novel series of gentiopicroside derivatives was designed and synthesized. All synthesized compounds were then biologically evaluated for their inhibition of influenza virus and anti-HCV activity in vitro. Some of the gentiopicroside derivatives, such as 11a, 13d and 16 showed interesting anti-influenza virus activity with IC[SUB]50[/SUB] at 39.5 μM, 45.2 μM and 44.0 μM, respectively. However, no significant anti-HCV activity was found for all of gentiopicroside derivatives. The preliminary results indicate that modification of the sugar moiety on gentiopicroside was helpful for enhancing the anti-influenza activities. Our works demonstrate the importance of secoiridoid natural products as new leads in the development of potential antiviral inhibitors.
Copyright ? 2017 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Anti-influenza virus; Antiviral agents; Gentiopicroside derivatives; Natural product; Secoiridoid
PMID: 28254701 DOI: 10.1016/j.ejmech.2017.02.028
[PubMed - as supplied by publisher]