Synthesis of Chimeric Thiazolo‐Nootkatone Derivatives as Potent Antimicrobial Agents
Ibrahim S. Alkhaibari, Hansa Raj K. C., Rawan Alnufaie, David F. Gilmore, Mohammad A. Alam
Abstract
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 μg/mL. The lead compound is bactericidal and very potent against S. aureus persisters. These compounds are nontoxic to human cancer cell lines at 10 μm concentration.
Topics & Concepts
AntimicrobialStaphylococcus aureusEnterococcus faeciumThiazoleChemistryMinimum inhibitory concentrationBacteriaNatural productCombinatorial chemistryMicrobiologyStereochemistryAntibioticsBiologyOrganic chemistryBiochemistryGeneticsSynthesis and biological activityMulticomponent Synthesis of HeterocyclesBioactive Compounds and Antitumor Agents