tetano
Editor, Senior Moderator
Molecules. 2019 Jul 17;24(14). pii: E2603. doi: 10.3390/molecules24142603.
[h=1]Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.[/h] Takeuchi T[SUP]1[/SUP], Sriwilaijaroen N[SUP]2,[/SUP][SUP]3[/SUP], Sakuraba A[SUP]4[/SUP], Hayashi E[SUP]4[/SUP], Kamisuki S[SUP]5[/SUP], Suzuki Y[SUP]3[/SUP], Ohrui H[SUP]6[/SUP], Sugawara F[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza A viruses leading to infectious respiratory diseases cause seasonal epidemics and sometimes periodic global pandemics. Viral polymerase is an attractive target in inhibiting viral replication, and 4'-ethynyladenosine, which has been reported as a highly potent anti-human immunodeficiency virus (HIV) nucleoside derivative, can work as an anti-influenza agent. Herein, we designed and synthesized a 4'-ethynyl-2'-deoxyadenosine 5'-monophosphate analog called EdAP (5). EdAP exhibited potent inhibition against influenza virus multiplication in Madin-Darby canine kidney (MDCK) cells transfected with human α2-6-sialyltransferase (SIAT1) cDNA and did not show any toxicity toward the cells. Surprisingly, this DNA-type nucleic acid analog (5) inhibited the multiplication of influenza A virus, although influenza virus is an RNA virus that does not generate DNA.
[h=4]KEYWORDS:[/h] 4′-ethynyl-2′-deoxyadenosine 5′-monophosphate; anti-influenza activity; influenza
PMID: 31319565 DOI: 10.3390/molecules24142603
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[h=1]Design, Synthesis, and Biological Evaluation of EdAP, a 4'-Ethynyl-2'-Deoxyadenosine 5'-Monophosphate Analog, as a Potent Influenza a Inhibitor.[/h] Takeuchi T[SUP]1[/SUP], Sriwilaijaroen N[SUP]2,[/SUP][SUP]3[/SUP], Sakuraba A[SUP]4[/SUP], Hayashi E[SUP]4[/SUP], Kamisuki S[SUP]5[/SUP], Suzuki Y[SUP]3[/SUP], Ohrui H[SUP]6[/SUP], Sugawara F[SUP]4[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Influenza A viruses leading to infectious respiratory diseases cause seasonal epidemics and sometimes periodic global pandemics. Viral polymerase is an attractive target in inhibiting viral replication, and 4'-ethynyladenosine, which has been reported as a highly potent anti-human immunodeficiency virus (HIV) nucleoside derivative, can work as an anti-influenza agent. Herein, we designed and synthesized a 4'-ethynyl-2'-deoxyadenosine 5'-monophosphate analog called EdAP (5). EdAP exhibited potent inhibition against influenza virus multiplication in Madin-Darby canine kidney (MDCK) cells transfected with human α2-6-sialyltransferase (SIAT1) cDNA and did not show any toxicity toward the cells. Surprisingly, this DNA-type nucleic acid analog (5) inhibited the multiplication of influenza A virus, although influenza virus is an RNA virus that does not generate DNA.
[h=4]KEYWORDS:[/h] 4′-ethynyl-2′-deoxyadenosine 5′-monophosphate; anti-influenza activity; influenza
PMID: 31319565 DOI: 10.3390/molecules24142603
Free full text