<i>Staphylococcus aureus</i> is found on human skin and mucous membranes. Approximately 15% of the population carries S. aureus in the anterior nares. Depending on the state of the immune system of each host, MRSA can cause a wide spectrum of diseases, ranging from minor skin infections to mortal pneumonia. During the past decades, much attention has been shown to the synthesis of new organo-metal complexes and the evaluation of these agents for antibacterial activity. It has been found that thiosemicarbazones represent a new promising class of antibiotics that are effective against an array of Methicillin-resistant Staphylococcus aureus strains (MRSA). We have recognized several classes of heterocyclic compounds with the extended version of the thiosemicarbazone core motif (NNSN), which show better antibacterial properties against MRSA in the presence of Cu(I) ions. Although the concentration of free copper ions in cells is virtually undetectable in mammalian bodies, the elevated level of Cu(I) ions can be found in phagosomes which accelerates the formation of Cu(I)-NNSN complexes inside the phagosome. Excessive levels of Cu(I) ions are known to inhibit the growth of MRSA. This presentation will deliver the update of the foremost recent synthetic strategies to enhance the antibacterial activities of our drug candidates in nanomolar concentrations.

Synthesis, characterization and evaluation of novel heterocyclic thiosemicarbazones against MRSA

2019 Fall National Meeting

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