Your browser doesn't support javascript.
Synthesis and evaluation of 3-alkynyl-5-aryl-7-aza-indoles as broad-spectrum antiviral agents.
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.
  • Martinez-Gualda B; KU Leuven, Department of Pharmaceutical and Pharmacological Sciences, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Leuven, Belgium.
  • Graus M; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Camps A; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Vanhulle E; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Saul S; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Azari S; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, CA, United States.
  • Nhu Tran DH; Department of Microbiology and Immunology, Stanford University, Stanford, CA, United States.
  • Vangeel L; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, CA, United States.
  • Chiu W; Department of Microbiology and Immunology, Stanford University, Stanford, CA, United States.
  • Neyts J; Department of Medicine, Division of Infectious Diseases and Geographic Medicine, Stanford University, Stanford, CA, United States.
  • Schols D; Department of Microbiology and Immunology, Stanford University, Stanford, CA, United States.
  • Einav S; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • Vermeire K; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
  • De Jonghe S; KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
Front Chem ; 10: 1058229, 2022.
Article in English | MEDLINE | ID: covidwho-2119726
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.
Keywords
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: Available Collection: International databases Database: MEDLINE Type of study: Experimental Studies Language: English Journal: Front Chem Year: 2022 Document Type: Article Affiliation country: Fchem.2022.1058229

Similar

MEDLINE
LILACS
LIS
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: Available Collection: International databases Database: MEDLINE Type of study: Experimental Studies Language: English Journal: Front Chem Year: 2022 Document Type: Article Affiliation country: Fchem.2022.1058229