Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors

VX-787 is a first in class, orally bioavailable compound that offers unparalleled potential for the treatment of pandemic and seasonal influenza. As a part of our routine SAR exploration, carboxylic acid isosteres of VX-787 were prepared and tested against influenza A. It was found that the negative...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-05, Vol.25 (9), p.1990-1994
Hauptverfasser:	Boyd, Michael J, Bandarage, Upul K, Bennett, Hamilton, Byrn, Randal R, Davies, Ioana, Gu, Wenxin, Jacobs, Marc, Ledeboer, Mark W, Ledford, Brian, Leeman, Joshua R, Perola, Emanuele, Wang, Tiansheng, Bennani, Youssef, Clark, Michael P, Charifson, Paul S
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology Aza Compounds - chemistry Aza Compounds - pharmacology Carboxylic Acids - chemistry Dose-Response Relationship, Drug Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Influenza A virus - drug effects Influenza A virus - enzymology Microbial Sensitivity Tests Molecular Structure Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship Viral Proteins - antagonists & inhibitors Viral Proteins - metabolism
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