Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents

ChemMedChem. 2021 May 6. doi: 10.1002/cmdc.202100230. Online ahead of print.ABSTRACTNootkatone, 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 (15 and 16) are found to be potent antimicrobial agents against Staphylococcus aureus and Enterococcus faecium with minimum inhibitory concentration (MIC) values as low as 1.56 µg/ml. The lead compound (16) is bactericidal and very potent against S. aureus persisters. These compounds are non-toxic to human cancer cell lines at higher concentrations.PMID:33955181 | DOI:10.1002/cmdc.202100230
Source: ChemMedChem - Category: Chemistry Authors: Source Type: research