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

ABSTRACT: 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.

SUBMITTER: Martinez-Gualda B

PROVIDER: S-EPMC9643853 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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

Martinez-Gualda Belén B Graus Mirthe M Camps Anita A Vanhulle Emiel E Saul Sirle S Azari Siavash S Nhu Tran Do Hoang DH Vangeel Laura L Chiu Winston W Neyts Johan J Schols Dominique D Einav Shirit S Vermeire Kurt K De Jonghe Steven S

Frontiers in chemistry 20221026

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-<i>b</i>]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 ...[more]

PMID: 36385995

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