Synthesis and biological evaluation of oxindoles and benzimidazolinones derivatives

  • Samir Messaoudi
  • , Martine Sancelme
  • , Valérie Polard-Housset
  • , Bettina Aboab
  • , Pascale Moreau
  • , Michelle Prudhomme

Research output: Contribution to journalArticlepeer-review

Abstract

The synthesis of new oxindoles and benzimidazolinones derivatives bearing a sugar residue on the aromatic nitrogen is described. The presence of the glycoside moiety should enhance the solubility of these heterocyclic compounds and/or improve the interaction with the active site of the biological targets. The inhibitory activities of these new compounds toward five kinases were examined: KDR (VEGFR-2), FGFR-1, PDGFR-β, EGFR and Tie 2. Furthermore, the antibacterial activities of the prepared compounds were tested against two Gram-positive bacteria Bacillus cereus and Streptomyces chartreusis, a Gram-negative bacterium Escherichia coli and a yeast Candida albicans.

Original languageEnglish
Pages (from-to)453-458
Number of pages6
JournalEuropean Journal of Medicinal Chemistry
Volume39
Issue number5
DOIs
Publication statusPublished - 1 May 2004
Externally publishedYes

Keywords

  • Antimicrobial agents
  • Benzimidazolinones
  • Kinases inhibitors
  • Oxindoles

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