tetano
Editor, Senior Moderator
Chem Biol Drug Des. 2015 Feb 10. doi: 10.1111/cbdd.12534. [Epub ahead of print]
[h=1]Targeting Influenza A virus RNA Promoter.[/h] Bottini A[SUP]1[/SUP], De SK, Wu B, Tang C, Varani G, Pellecchia M.
[h=3]Author information[/h]
[h=3]Abstract[/h] The emergence of drug-resistant strains of influenza virus, makes exploring new classes of inhibitors that target universally conserved viral targets a highly important goal. The influenza A viral genome is made up of 8 single-stranded RNA negative segments. The RNA promoter, consisting of the conserved sequences at the 3' and 5' end of each RNA genomic segment, is universally conserved among influenza A virus strains and in all segments. Previously we reported on the identification and NMR structure of DPQ (6,7-dimethoxy-2-(1-piperazinyl)-4-quinazolinamine) (compound 1) in complex with the RNA promoter. Here we report on additional screening and SAR studies with compound 1, including ex vivo anti-influenza activity assays, resulted in improved cellular activity against influenza A virus in the micromolar range. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
PMID: 25676805 [PubMed - as supplied by publisher]
[h=1]Targeting Influenza A virus RNA Promoter.[/h] Bottini A[SUP]1[/SUP], De SK, Wu B, Tang C, Varani G, Pellecchia M.
[h=3]Author information[/h]
[h=3]Abstract[/h] The emergence of drug-resistant strains of influenza virus, makes exploring new classes of inhibitors that target universally conserved viral targets a highly important goal. The influenza A viral genome is made up of 8 single-stranded RNA negative segments. The RNA promoter, consisting of the conserved sequences at the 3' and 5' end of each RNA genomic segment, is universally conserved among influenza A virus strains and in all segments. Previously we reported on the identification and NMR structure of DPQ (6,7-dimethoxy-2-(1-piperazinyl)-4-quinazolinamine) (compound 1) in complex with the RNA promoter. Here we report on additional screening and SAR studies with compound 1, including ex vivo anti-influenza activity assays, resulted in improved cellular activity against influenza A virus in the micromolar range. This article is protected by copyright. All rights reserved.
This article is protected by copyright. All rights reserved.
PMID: 25676805 [PubMed - as supplied by publisher]