tetano
Editor, Senior Moderator
Bioorg Med Chem. 2016 Apr 5. pii: S0968-0896(16)30244-9. doi: 10.1016/j.bmc.2016.04.010. [Epub ahead of print]
[h=1]1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.[/h] Geisman AN[SUP]1[/SUP], Valuev-Elliston VT[SUP]2[/SUP], Ozerov AA[SUP]1[/SUP], Khandazhinskaya AL[SUP]2[/SUP], Chizhov AO[SUP]3[/SUP], Kochetkov SN[SUP]2[/SUP], Pannecouque C[SUP]4[/SUP], Naesens L[SUP]4[/SUP], Seley-Radtke KL[SUP]5[/SUP], Novikov MS[SUP]1[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of 1,6-bis[(benzyloxy)methyl]uracil derivatives combining structural features of both diphenyl ether and pyridone types of NNRTIs were synthesized. Target compounds were found to inhibit HIV-1 reverse transcriptase at micro- and submicromolar levels of concentrations and exhibited anti-HIV-1 activity in MT-4 cell culture, demonstrating resistance profile similar to first generation NNRTIs. The synthesized compounds also showed profound activity against influenza virus (H1N1) in MDCK cell culture without detectable cytotoxicity. The lead compound of this assay appeared to exceed rimantadine, amantadine, ribavirin and oseltamivir carboxylate in activity. The mechanism of action of 1,6-bis[(benzyloxy)methyl]uracils against influenza virus is currently under investigation.
Copyright ? 2016 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] HIV; Influenza virus; NNRTIs; Non-nucleoside reverse transcriptase inhibitors; Uracil
PMID: 27112451 [PubMed - as supplied by publisher]
[h=1]1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.[/h] Geisman AN[SUP]1[/SUP], Valuev-Elliston VT[SUP]2[/SUP], Ozerov AA[SUP]1[/SUP], Khandazhinskaya AL[SUP]2[/SUP], Chizhov AO[SUP]3[/SUP], Kochetkov SN[SUP]2[/SUP], Pannecouque C[SUP]4[/SUP], Naesens L[SUP]4[/SUP], Seley-Radtke KL[SUP]5[/SUP], Novikov MS[SUP]1[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of 1,6-bis[(benzyloxy)methyl]uracil derivatives combining structural features of both diphenyl ether and pyridone types of NNRTIs were synthesized. Target compounds were found to inhibit HIV-1 reverse transcriptase at micro- and submicromolar levels of concentrations and exhibited anti-HIV-1 activity in MT-4 cell culture, demonstrating resistance profile similar to first generation NNRTIs. The synthesized compounds also showed profound activity against influenza virus (H1N1) in MDCK cell culture without detectable cytotoxicity. The lead compound of this assay appeared to exceed rimantadine, amantadine, ribavirin and oseltamivir carboxylate in activity. The mechanism of action of 1,6-bis[(benzyloxy)methyl]uracils against influenza virus is currently under investigation.
Copyright ? 2016 Elsevier Ltd. All rights reserved.
[h=4]KEYWORDS:[/h] HIV; Influenza virus; NNRTIs; Non-nucleoside reverse transcriptase inhibitors; Uracil
PMID: 27112451 [PubMed - as supplied by publisher]