2. Academic Validation
  3. Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents

Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents

  • ChemMedChem. 2021 Sep 6;16(17):2628-2637. doi: 10.1002/cmdc.202100230.
Ibrahim S Alkhaibari 1,  Hansa Raj K C 1,  Rawan Alnufaie 1,  David Gilmore 2,  Mohammad A Alam 1
Affiliations

Affiliations

  • 1 Department of Chemistry and Physics, College of Science and Mathematics, Arkansas State University, 72467, Jonesboro, AR, USA.
  • 2 Department of Biological Sciences, College of Science and Mathematics, Arkansas State University, 72467, Jonesboro, AR, USA.
PMID: 33955181 DOI: 10.1002/cmdc.202100230
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.

Keywords

MRSA; Nootkatone; chimeric compounds; persisters; thiazole.

Figures
Products