Authors: J. Vinšová; A. Imramovský Authors‘ workplace: Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové Published in: Čes. slov. Farm., 2004; , 294-299 Category:
The review presents a survey of potential biologically active salicylanilides, focusing particularly ontheir antibacterial activity. Emergence of bacterial resistance to a large number of antibacterialagents represents a major world-wide problem. On that account, perpetual attention is paid to thepreparation of new bioactive antibacterial compounds. Salicylanilides belong to the group ofcompounds that have shown activity against gram-positive pathogens including methicillin-resistantStaphylococcus aureus and vancomycin-resistant Enterococcus faecium, the strains representingthe most significant problem in clinical practice. In 1998, a new mechanism of their actionwas proposed. Salicylanilides are inhibitors of two-component regulatory systems in bacteria.Electron-accepting substituents on the salicylic and hydrophobic groups on the anilide ring are mostessential for the activity, but other electronic and structural parameters may also play an importantrole. Our aim, based on SAR analysis, is to develop new active drugs esterified by amino acid andlater peptides. Furthermore, analogues carrying the hydroxybenzamide moiety may uncoupleoxidative phosphorylation.
Key words: salicylanilides – pharmacophore – biological activity – antibacterial activity
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