AUTHOR=Martinez-Gualda Belén , Graus Mirthe , Camps Anita , Vanhulle Emiel , Saul Sirle , Azari Siavash , Nhu Tran Do Hoang , Vangeel Laura , Chiu Winston , Neyts Johan , Schols Dominique , Einav Shirit , Vermeire Kurt , De Jonghe Steven 

TITLE=Synthesis and evaluation of 3-alkynyl-5-aryl-7-aza-indoles as broad-spectrum antiviral agents

JOURNAL=Frontiers in Chemistry

VOLUME=10

YEAR=2022

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2022.1058229

DOI=10.3389/fchem.2022.1058229

ISSN=2296-2646

ABSTRACT=<p>RNA viral infections, including those caused by respiratory syncytial virus (RSV), severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), and Venezuelan Equine encephalitis virus (VEEV), pose a major global health challenge. Here, we report the synthesis and screening of a series of pyrrolo[2,3-<italic>b</italic>]pyridines targeting RSV, SARS-CoV-2 and/or VEEV. From this campaign, a series of lead compounds was generated that demonstrated antiviral activity in the low single-digit micromolar range against the various viruses and did not show cytotoxicity. These findings highlight the potential of 3-alkynyl-5-aryl-7-aza-indoles as a promising chemotype for the development of broad-spectrum antiviral agents.</p>