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.

Document Details

Document Type
Pub Defense Publication
Publication Date
Oct 26, 2022
Source ID
10.3389/fchem.2022.1058229

Entities

People

  • Anita Camps
  • BelĂ©n Martinez-gualda
  • Do Hoang Nhu Tran
  • Dominique Schols
  • Emiel Vanhulle
  • Johan Neyts
  • Kurt Vermeire
  • Laura Vangeel
  • Mirthe Graus
  • Shirit Einav
  • Siavash Azari
  • Sirle Saul
  • Steven De Jonghe
  • Winston Chiu

Organizations

  • Defense Threat Reduction Agency
  • National Institute of Allergy and Infectious Diseases
  • United States Department of Defense

Tags

Readers

  • Virology (or Medical Virology).