Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents

Nootkatone, an approved insecticide, is a well-known natural product from grapefruit. A series of fused-thiazole derivatives of nootkatone have been synthesized, and these new compounds were tested against several strains of bacteria. Some of these compounds are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 mu g/mL. The lead compound is bactericidal and very potent against S. aureus persisters. These compounds are nontoxic to human cancer cell lines at 10 mu m concentration.

Automated summary

Synthesized fused-thiazole derivatives of nootkatone showed potent antimicrobial activity against Staphylococcus aureus and Enterococcus faecium, while being non-toxic to human cancer cell lines.