Tiosemikarbazonowe pochodne p-bromo acetofenonu jako inhibitory bakteryjnych metalo-β-laktamaz

β-lactamases are responsible for bacterial resistance to β-lactam antibiotics through their ability to inactivate the β-lactam ring. The NDM-1 enzyme belongs to metallo-β-lactamases for which no effective agents inhibiting their activity have been developed. However, three compounds in the second clinical trial can effectively inactivate NDM-1, but those clinical trials are connected with their anticancer properties. Because of the still pressing problem related to the search for effective inhibitors of Metallo-β-lactamases, an attempt was made to determine the most effective inhibitor among the tested thiosemicarbazone analogs of acetophenone. The results of screening tests conducted on Escherichia coli containing plasmid pET-15b coding NDM-1 correlated with molecular docking results. The results indicate that the most effective inhibitor among the compounds tested is the derivative containing a phenyl and methyl group in positions R1 and R2, respectively, and a phenyl ring in position R3.