Syntheses of Isatins and Oxindoles Derivatives as SARS-CoV-2 Inhibitors Evaluated through Phenotypic Screening with Vero Cells

Publikationstyp:
Zeitschriftenaufsatz
Metadaten:
Autoren
  • Cintia MCF Lima
  • Lucio H Freitas-Junior
  • Carolina B Moraes
  • Cecilia G Barbosa
  • Till Opatz
  • Mauricio M Victor
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000886223900001&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.21577/0103-5053.20220138
eISSN
1678-4790
Externe Identifier
  • Clarivate Analytics Document Solution ID: 6I6FL
ISSN
0103-5053
Zeitschrift
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
Schlüsselwörter
  • 3-hydroxy bis-oxindoles
  • isoindigos
  • isatins
  • SARS-CoV-2
  • phenotypic VERO essay
Datum der Veröffentlichung
2022
Status
Published
Titel
Syntheses of Isatins and Oxindoles Derivatives as SARS-CoV-2 Inhibitors Evaluated through Phenotypic Screening with Vero Cells
Sub types
  • Article
  • Early Access

Datenquelle: Web of Science (Lite)

Andere Metadatenquellen:
Abstract
<jats:p>To expand the variety of density functionalized compounds evaluated against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), we decided to prepare new acetylated and disubstituted 3-hydroxy bis-oxindoles and isoindigos coupling compounds using known protocols. The corresponding isatin derivatives were synthesized by ZrCl4/EtOH/reflux or HCl/AcOH/ reflux coupling conditions using oxindole and functionalized isatins, furnishing new 3-hydroxy bis-oxindoles, which were dehydrated into new isoindigos. A total of 27 compounds bearing halogen, nitro and/or hydroxy groups on the isatin moiety, at the 3-, 5- and 7-positions, were prepared, including 5 new 3-hydroxy bis-oxindoles and 3 new halogenated isoindigos prepared according adapted procedures described in the literature. This library of nitrogen-isatin derivatives was evaluated against SARS-CoV-2 using a phenotypic screening assay. In this investigation, isatin derivatives 3d, 3e, 3h and 3i showed antiviral activity when tested at a single concentration. Compound 3e showed antiviral activity against SARS-CoV-2 in the concentration-response assay, however, it showed cellular toxicity in Vero cells. The present study identified substituted isatins as a promising new starting point for the development of anti-SARS-CoV-2 agents.</jats:p>
Autoren
  • Cintia Lima
  • Lúcio Freitas-Junior
  • Carolina Moraes
  • Cecília Barbosa
  • Till Opatz
  • Mauricio Victor
DOI
10.21577/0103-5053.20220138
ISSN
0103-5053
Zeitschrift
Journal of the Brazilian Chemical Society
Online publication date
2023
Status
Published online
Herausgeber
Sociedade Brasileira de Quimica (SBQ)
Herausgeber URL
http://dx.doi.org/10.21577/0103-5053.20220138
Datum der Datenerfassung
2022
Titel
Synthesis of Isatins and Oxindoles Derivatives as SARS-CoV-2 Inhibitors Evaluated through Phenotypic Screening with Vero Cells

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