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

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...

Descripción completa

Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9643853/
https://www.ncbi.nlm.nih.gov/pubmed/36385995
http://dx.doi.org/10.3389/fchem.2022.1058229
Descripción
Sumario: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.

Ejemplares similares