Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5605-5609
2006
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Details
- Autor(en) / Beteiligte
- Titel
- Sesquiterpene lactones are potent and irreversible inhibitors of the antibacterial target enzyme MurA
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2006-11, Vol.16 (21), p.5605-5609
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2006
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- Certain sesquiterpene lactones are potent inhibitors of the antibacterial target enzyme MurA. We present structure–activity relationships and discuss biological implications. We report the identification of the sesquiterpene lactones cnicin and cynaropicrin as potent, irreversible inhibitors of the bacterial enzyme MurA. They covalently bind to the thiol group of Cys115. Judging from the structure–activity relationships, we conclude that the unsaturated ester side chain of cynaropicrin and cnicin is of particular importance for the inhibition of MurA. These results provide evidence that MurA is a target protein of SLs with a probably high relevance for their known antibacterial effect.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/j.bmcl.2006.08.021Titel-ID: cdi_proquest_miscellaneous_68878611
- Format
- –
- Schlagworte
- Alkyl and Aryl Transferases - antagonists & inhibitors, Antibacterial agents, Antibiotic, Antibiotics. Antiinfectious agents. Antiparasitic agents, Biological and medical sciences, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, Escherichia coli - drug effects, Escherichia coli - enzymology, Lactones - chemistry, Lactones - pharmacology, Medical sciences, MurA, Peptidoglycan - biosynthesis, Pharmacology. Drug treatments, Pseudomonas aeruginosa - drug effects, Pseudomonas aeruginosa - enzymology, Sesquiterpene lactones, Sesquiterpenes - chemistry, Sesquiterpenes - pharmacology, Structure-Activity Relationship, Structure–activity relationships