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GRAPHICAL ABSTRACT
ABSTRACT
Metallo-β-lactamases (MβLs) are the target enzymes of antibiotic resistance and the phosphonic drugs make great influence to the development of contemporary medicine. Eleven acetamidophosphonic compounds were prepared and evaluated as inhibitors of the MβLs. Compounds 4, 5, 7, 9, and 10 exhibited specific inhibitory activity against the MβL NDM-1 and CcrA with an IC50 value range of 17 to 354 μM. Analysis of the structure–activity relationship showed that both the acetamido linker and the position of the substituent on the phenyl ring played an important role in the inhibitory abilities of the inhibitors against MβLs.
Funding
This work was financially supported by grants 81361138018, 21272186, and 21572179 (to K.W.Y.) from the National Natural Science Foundation of China.