tetano
Editor, Senior Moderator
Carbohydr Res. 2019 Apr 1;477:32-38. doi: 10.1016/j.carres.2019.03.012. [Epub ahead of print]
[h=1]Divalent oseltamivir analogues as potent influenza neuraminidase inhibitors.[/h] Yan ZL[SUP]1[/SUP], Liu AY[SUP]2[/SUP], Wei XX[SUP]2[/SUP], Zhang Z[SUP]2[/SUP], Qin L[SUP]2[/SUP], Yu Q[SUP]2[/SUP], Yu P[SUP]2[/SUP], Lu K[SUP]3[/SUP], Yang Y[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A panel of divalent oseltamivir and guanidino oseltamivir analogues with esterification on the carboxyl acid group as potent inhibitors of influenza virus neuraminidase was prepared via click reaction. The primary structure activity relationship study demonstrated that appropriate distance between two oseltamivir monomers around 30 ? can crosslink two adjacent neuraminidase tetramers on the virion surface and result in highly effective NA inhibitors against three strains of influenza virus and H7N9 virus like particle. This strategy also provides a basis for the multivalent modification on oseltamivir.
Copyright ? 2019 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] Click chemistry; Cluster effect; Neuraminidase inhibitor; Oseltamivir guanidino oseltamivir
PMID: 30954773 DOI: 10.1016/j.carres.2019.03.012
[h=1]Divalent oseltamivir analogues as potent influenza neuraminidase inhibitors.[/h] Yan ZL[SUP]1[/SUP], Liu AY[SUP]2[/SUP], Wei XX[SUP]2[/SUP], Zhang Z[SUP]2[/SUP], Qin L[SUP]2[/SUP], Yu Q[SUP]2[/SUP], Yu P[SUP]2[/SUP], Lu K[SUP]3[/SUP], Yang Y[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A panel of divalent oseltamivir and guanidino oseltamivir analogues with esterification on the carboxyl acid group as potent inhibitors of influenza virus neuraminidase was prepared via click reaction. The primary structure activity relationship study demonstrated that appropriate distance between two oseltamivir monomers around 30 ? can crosslink two adjacent neuraminidase tetramers on the virion surface and result in highly effective NA inhibitors against three strains of influenza virus and H7N9 virus like particle. This strategy also provides a basis for the multivalent modification on oseltamivir.
Copyright ? 2019 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] Click chemistry; Cluster effect; Neuraminidase inhibitor; Oseltamivir guanidino oseltamivir
PMID: 30954773 DOI: 10.1016/j.carres.2019.03.012