[Salicylanilides: still a potential antibacterially active group].
The review presents a survey of potential biologically active salicylanilides, focusing particularly on their antibacterial activity. Emergence of bacterial resistance to a large number of antibacterial agents represents a major world-wide problem. On that account, perpetual attention is paid to the preparation of new bioactive antibacterial compounds. Salicylanilides belong to the group of compounds that have shown activity against gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium, the strains representing the most significant problem in clinical practice. In 1998, a new mechanism of their action was 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 most essential for the activity, but other electronic and structural parameters may also play an important role. Our aim, based on SAR analysis, is to develop new active drugs esterified by amino acid and later peptides. Furthermore, analogues carrying the hydroxybenzamide moiety may uncouple oxidative phosphorylation.
Vinsová
J
J
Katedra anorganické a organické chemie Farmaceutické fakulty Univerzity Karlovy, Hradec Králové. vinsova@faf.cuni.cz
Imramovský
A
A
D000900:Anti-Bacterial Agents / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D012458:Salicylanilides / Q000737:chemistry / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D012458:Salicylanilides