Synthesis and biological evaluation of oxindoles and benzimidazolinones derivatives.
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-beta, 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.
Messaoudi
Samir
S
Laboratoire SEESIB, Université Blaise Pascal, UMR 6504 du CNRS, 24, avenue des Landais, 63177 Aubière cedex, France.
Sancelme
Martine
M
Polard-Housset
Valérie
V
Aboab
Bettina
B
Moreau
Pascale
P
Prudhomme
Michelle
M
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010770:Phosphotransferases / Q000037:antagonists & inhibitors*
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D001562:Benzimidazoles; D007211:Indoles; D010770:Phosphotransferases