Synthesis of Chimeric Thiazolo-Nootkatone Derivatives as Potent Antimicrobial Agents.
MRSA
Nootkatone
chimeric compounds; persisters
thiazole
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
06 09 2021
06 09 2021
Historique:
received:
01
04
2021
pubmed:
7
5
2021
medline:
26
2
2022
entrez:
6
5
2021
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 33955181
doi: 10.1002/cmdc.202100230
pmc: PMC8429137
mid: NIHMS1707401
doi:
Substances chimiques
Anti-Bacterial Agents
0
Polycyclic Sesquiterpenes
0
Thiazoles
0
nootkatone
IZ2Y119N4J
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
2628-2637Subventions
Organisme : Research Technology Core of the Arkansas INBRE program
Organisme : NIGMS NIH HHS
ID : P20 GM103429
Pays : United States
Informations de copyright
© 2021 Wiley-VCH GmbH.
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