1245569-76-9Relevant articles and documents
Cinnamonitrile adjuvants restore susceptibility to β-lactams against methicillin-resistant staphylococcus aureus
Speri, Enrico,Kim, Choon,De Benedetti, Stefania,Qian, Yuanyuan,Lastochkin, Elena,Fishovitz, Jennifer,Fisher, Jed F.,Mobashery, Shahriar
supporting information, p. 1148 - 1153 (2019/08/27)
β-Lactams are used routinely to treat Staphylococcus aureus infections. However, the emergence of methicillin-resistant S. aureus (MRSA) renders them clinically precarious. We describe a class of cinnamonitrile adjuvants that restore the activity of oxacillin (a penicillin member of the β-lactams) against MRSA. The lead adjuvants were tested against six important strains of MRSA, one vancomycin-intermediate S. aureus (VISA) strain, and one linezolid-resistant S. aureus strain. Five compounds out of 84 total compounds showed broad potentiation. At 8 μM (E)-3-(5-(3,4-dichlorobenzyl)-2-(trifluoromethoxy)phenyl)-2-(methylsulfonyl)acrylonitrile (26) potentiated oxacillin with a >4000-fold reduction of its MIC (from 256 to 0.06 mg·L-1). This class of adjuvants holds promise for reversal of the resistance phenotype of MRSA.
