Therefore, the development of novel types of antistaphylococcal agents is of great importance. aureus (VISA and VRSA) strains remain serious medical and public problems worldwide since the antibiotics of the last choice such as linezolid, teicoplanin and daptomycin are not always effective and have shown a tendency to lose their effectiveness due to resistance. Nowadays, methicillin- (MRSA) and vancomycin-resistant S. The main problem of staphylococcal infections treatment is the increasing emergence of multidrug resistance.
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aureus) is one of the most common nosocomial pathogens that causes a number of hospital-acquired diseases ranging from skin infections to severe human infections associated with high levels of morbidity and mortality such as sepsis, endocarditis, osteomyelitis, necrotizing pneumonia, etc. aureus ATCC strains was also observed suggesting that the compound reduced biofilm formation by changing the biofilm structure and thickness. The effect of the compound on biofilms produced by two S. Antibacterial and antibiofilm assays also confirmed high specificity of the hit compound against two standard and three wild-type, S. Microscale thermophoresis experiments confirmed that this compound bound sortase A with K D value of 189 µM. This compound was selective toward sortase A compared to other four cysteine proteases – cathepsin L, cathepsin B, rhodesain, and the SARS-CoV2 main protease. aureus sortase A at the IC 50 value of 59.7 µM.
The most promising compound was 2-(2-amino-3-chloro-benzoylamino)-benzoic acid which was able to inhibit S. Using hybrid virtual screening approach and FRET analysis, we have identified five compounds able to decrease the activity of sortase A by more than 50% at the concentration of 200 µM. Sortase A is considered as a promising molecular target for the development of antistaphylococcal agents. Staphylococcus aureus is one of the most dangerous pathogens commonly associated with high levels of morbidity and mortality.