Discovery of a Macrocyclic Influenza Cap-Dependent Endonuclease Inhibitor.

Influenza viruses (IFVs) have caused several pandemics and have claimed numerous lives since their first record in the early 20th century. While the outbreak of COVID-19 seemed to expel influenza from the sight of people for a short period of time, it is not surprising that it will recirculate around the globe after the coronavirus has mutated into a less fatal variant. Baloxavir marboxil (), the prodrug of baloxavir () and a cap-dependent endonuclease (CEN) inhibitor, were approved by the FDA for the first treatment in almost 20 years.

Correction to "The Discovery of 3,3'-Spiro[azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection".

[This corrects the article DOI: 10.1021/acsmedchemlett.7b00418.

Discovery of 3,3'-Spiro[Azetidine]-2-oxo-indoline Derivatives as Fusion Inhibitors for Treatment of RSV Infection.

A new series of 3,3'-spirocyclic-2-oxo-indoline derivatives was synthesized and evaluated against respiratory syncytial virus (RSV) in a cell-based assay and animal model. Extensive structure-activity relationship study led to a lead compound , which exhibited excellent potency with an EC value of 0.8 nM and demonstrated 71% oral bioavailability in mice.