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

Autor: Belén Martinez-Gualda, Mirthe Graus, Anita Camps, Emiel Vanhulle, Sirle Saul, Siavash Azari, Do Hoang Nhu Tran, Laura Vangeel, Winston Chiu, Johan Neyts, Dominique Schols, Shirit Einav, Kurt Vermeire, Steven De Jonghe
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Frontiers in Chemistry, Vol 10 (2022)
Druh dokumentu: article
ISSN: 2296-2646
DOI: 10.3389/fchem.2022.1058229
Popis: 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.
Databáze: Directory of Open Access Journals