Sorafenib analog with unique antibacterial properties
Molekulargewicht:
394.68
Reinheit:
99% by HPLC NMR (Conforms)
Formulierung:
White solid
CAS Nummer:
[2165324-62-7]
Formel:
C15H8ClF5N2O3
Anwendungsbeschreibung:
PK150 is a Sorafenib analog that displays significant antibacterial activity against several pathogenic strains (S.aureus NCTC8325, MIC = 0.3 µM, vancomycin -resistant enterococci, MIC = 3 µM, and M.tuberculosis MIC = 2 µM). It was inactive against Gram-negative bacteria. It effectively reduced persister cells in ciprofloxacin-treated stationary S.aureus cultures and effectively eradicated staphylococcus biofilms. PK150 did not develop antibacterial resistance in an agar-plate-based assay. Its antibacterial properties were attributed to demethylmenaquinone methyltransferase (MenG) inhibition and signal peptidase IB (SpsB) activation. PK150 displayed in vivo efficacy in a murine bloodstream infection model against methicillin-sensitive S. aureus and a neutropenic mouse thigh model against methicillin-resistant S. aureus strain ATCC33591. Inactive against a panel of over 250 human kinases.
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