Synthesis and biological evaluation of oxindoles and benzimidazolines derivatives

Samir Messaoudi (1) , Martine Sancelme (1) , Valérie Polard-Housset (2) , Bettina Aboab (1) , Pascale Moreau (1) , Michelle Prudhomme (1)

1 SEESIB - Synthèse et étude de systèmes à intêret biologique
2 Aventis Pharma

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

Mots clés: Oxindoles; Benzimidazolinones; Kinases inhibitors; Antimicrobial agents

Domaines: Chimie organique

Samir Messaoudi, Martine Sancelme, Valérie Polard-Housset, Bettina Aboab, Pascale Moreau, et al.. Synthesis and biological evaluation of oxindoles and benzimidazolines derivatives. European Journal of Medicinal Chemistry, 2004, 39, pp.453-458. ⟨10.1016/j.ejmech.2004.01.001⟩. ⟨hal-00136184⟩