tetano
Editor, Senior Moderator
Chem Biol Drug Des. 2015 May 27. doi: 10.1111/cbdd.12589. [Epub ahead of print]
[h=1]2-Pyridinyl-4(3H)-quinazolinone: A Scaffold for Anti-influzenza A Virus Compounds.[/h] Liu S[SUP]1[/SUP], Wang W[SUP]1[/SUP], Jiang L[SUP]1[/SUP], Wan S[SUP]1[/SUP], Zhang L[SUP]1[/SUP], Yu R[SUP]1[/SUP], Jiang T[SUP]1[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of 2-pyridinyl-3-substituted-4(3H)-quinazolinones were synthesized and their anti-influenza A virus activities were determined using the cytopathic effect inhibition assay. Most of the compounds were potent with IC[SUB]50[/SUB] values ranging from 51.6 μM to 93.0 μM, which are better than that of the currently marketed drug Ribavirin. The molecular mechanisms of the new compounds were investigated using neuraminidase inhibition assay, cellular NF-κB signaling pathway inhibition assay and computational docking. Compound 4e, which is a- N3 imidazol-1-ylpropyl substituted derivative of 2-pyridinyl-4(3H)-quinazolinone, had the most potent anti-influenza A virus activity in vitro, and inhibited both virus neuraminidase and cellular NF-κB signaling pathway. In conclusion, 2-pyridinyl-4(3H)-quinazolinone is a new scaffold for the design of potent anti-influenza A virus compounds, offering an alternative approach to tackle influenza drug resistance. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
[h=4]KEYWORDS:[/h] 4(3H)-quinazolinone; Anti-influenza A; NF-κB signaling pathway; Neuraminidase; molecular docking
PMID: 26017319 [PubMed - as supplied by publisher]
[h=1]2-Pyridinyl-4(3H)-quinazolinone: A Scaffold for Anti-influzenza A Virus Compounds.[/h] Liu S[SUP]1[/SUP], Wang W[SUP]1[/SUP], Jiang L[SUP]1[/SUP], Wan S[SUP]1[/SUP], Zhang L[SUP]1[/SUP], Yu R[SUP]1[/SUP], Jiang T[SUP]1[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] A series of 2-pyridinyl-3-substituted-4(3H)-quinazolinones were synthesized and their anti-influenza A virus activities were determined using the cytopathic effect inhibition assay. Most of the compounds were potent with IC[SUB]50[/SUB] values ranging from 51.6 μM to 93.0 μM, which are better than that of the currently marketed drug Ribavirin. The molecular mechanisms of the new compounds were investigated using neuraminidase inhibition assay, cellular NF-κB signaling pathway inhibition assay and computational docking. Compound 4e, which is a- N3 imidazol-1-ylpropyl substituted derivative of 2-pyridinyl-4(3H)-quinazolinone, had the most potent anti-influenza A virus activity in vitro, and inhibited both virus neuraminidase and cellular NF-κB signaling pathway. In conclusion, 2-pyridinyl-4(3H)-quinazolinone is a new scaffold for the design of potent anti-influenza A virus compounds, offering an alternative approach to tackle influenza drug resistance. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
[h=4]KEYWORDS:[/h] 4(3H)-quinazolinone; Anti-influenza A; NF-κB signaling pathway; Neuraminidase; molecular docking
PMID: 26017319 [PubMed - as supplied by publisher]