Synthesis and Biological Evaluation of New Isatin-Based QACs with High Antimicrobial Potency

摘要

abstract_textpA simple and easy condensation reaction of aryl- or N-substituted isatins with Girard's reagents P and T was found to be useful in obtaining of water-soluble isatin-based quaternary ammonium compounds (QACs) bearing pyridinium or trimethylammonium moiety with high yields. Their antimicrobial activity was evaluated. Selective activity against Gram-positive bacteria (S. aureus 209p and B. cereus 8035) and yeast-like fungus Candida albicans 855-653 was shown. The influence of the substituent's nature as in the aromatic fragment as at position 1 on the activity was established. The most active are the pyridinium salts containing sterically hindered phenolic fragment at the position 1 of the heterocycle. The structures of all novel compounds were fully characterized using IR and NMR spectroscopies as well as XRD analysis./p/abstract_text