Discovery and synthesis of novel benzofurazan derivatives as inhibitors of influenza A virus.

Abstract

The identification of a novel hit compound inhibitor of the protein-protein interaction between the influenza RNA-polymerase PA and PB1 subunits has been accomplished by means of high-throughput screening. A small family of structurally related molecules has been synthesized and biologically evaluated with most of the compounds showing micromolar potency of inhibition against viral replication.

• Authors: Ulrich Kessler, Daniele Castagnolo, Mafalda Pagano, Davide Deodato, Martina Bernardini, Beatrice Pilger, Charlene Ranadheera, Maurizio Botta
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 23 Issue 20 Pg. 5575-7 (Oct 15 2013) ISSN: 1464-3405 [Electronic] England
• PMID: 24012120 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Ltd. All rights reserved.

Chemical References

• Antiviral Agents
• Benzoxazoles
• Enzyme Inhibitors
• Protein Subunits
• benzofurazan
• DNA-Directed RNA Polymerases

Topics

• Animals
• Antiviral Agents (chemical synthesis, chemistry, toxicity)
• Benzoxazoles (chemical synthesis, chemistry, toxicity)
• DNA-Directed RNA Polymerases (chemistry, metabolism)
• Dogs
• Drug Evaluation, Preclinical
• Enzyme Inhibitors (chemical synthesis, chemistry, toxicity)
• Influenza A virus (drug effects, enzymology)
• Madin Darby Canine Kidney Cells
• Protein Interaction Domains and Motifs (drug effects)
• Protein Subunits (chemistry, metabolism)
• Structure-Activity Relationship