tetano
Editor, Senior Moderator
Eur J Med Chem. 2016 Jan 4;109:199-205. doi: 10.1016/j.ejmech.2015.12.031. [Epub ahead of print]
[h=1]Design, synthesis, and biological evaluation of crenatoside analogues as novel influenza neuraminidase inhibitors.[/h] Chen BL[SUP]1[/SUP], Wang YJ[SUP]2[/SUP], Guo H[SUP]1[/SUP], Zeng GY[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Natural products, especially derived from TCMH, have been found to exert antiviral effects against influenza virus. Crenatoside, a phenylethanoid glycoside from Pogostemon cablin Benth, which has been shown as a novel effective NA inhibitor previously, is considered as the leading compound for our further SARs studies. This work presented design, synthesis of novel crenatoside analogues from readily available d-Glucose and l-rhamnose in a convergent manner. Furthermore, their biological activities and SARs were also investigated. Especially, compound 2 h showed impressive IC[SUB]50[/SUB] = 27.77 μg/mL against NAs, which is 3 folds more potent than the leading compound crenatoside (IC[SUB]50[/SUB] = 89.81 μg/mL). These results would promise their therapeutic potential for influenza disease.
Copyright ? 2016 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Crenatoside derivatives; Design; Influenza virus; Neuraminidases inhibitors; Synthesis
PMID: 26774928 [PubMed - as supplied by publisher]
[h=1]Design, synthesis, and biological evaluation of crenatoside analogues as novel influenza neuraminidase inhibitors.[/h] Chen BL[SUP]1[/SUP], Wang YJ[SUP]2[/SUP], Guo H[SUP]1[/SUP], Zeng GY[SUP]3[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Natural products, especially derived from TCMH, have been found to exert antiviral effects against influenza virus. Crenatoside, a phenylethanoid glycoside from Pogostemon cablin Benth, which has been shown as a novel effective NA inhibitor previously, is considered as the leading compound for our further SARs studies. This work presented design, synthesis of novel crenatoside analogues from readily available d-Glucose and l-rhamnose in a convergent manner. Furthermore, their biological activities and SARs were also investigated. Especially, compound 2 h showed impressive IC[SUB]50[/SUB] = 27.77 μg/mL against NAs, which is 3 folds more potent than the leading compound crenatoside (IC[SUB]50[/SUB] = 89.81 μg/mL). These results would promise their therapeutic potential for influenza disease.
Copyright ? 2016 Elsevier Masson SAS. All rights reserved.
[h=4]KEYWORDS:[/h] Crenatoside derivatives; Design; Influenza virus; Neuraminidases inhibitors; Synthesis
PMID: 26774928 [PubMed - as supplied by publisher]