期刊
CHEMMEDCHEM
卷 16, 期 17, 页码 2628-2637出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100230
关键词
Nootkatone; MRSA; thiazole; chimeric compounds; persisters
资金
- National Institute of General Medical Sciences (NIGMS) [P20GM103429]
- Kays Foundation
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.
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.
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