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

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

Format: Article
Diterbitkan: Frontiers Media S.A. 2022-10-01

Deskripsi

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-b]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.