کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1397225 | 1501114 | 2015 | 12 صفحه PDF | دانلود رایگان |
• Novel compounds with antimicrobial and fast anti-biofilm activity against Staphylococcus aureus.
• Facile, unusual and d-amino acid-based design to resist proteolysis.
• Very high potency against pre-formed biofilms when compared to common antibiotics.
• New chemical probes to study biofilms and leads to develop anti-infective drugs.
The combination of the dehydroabietic acid scaffold with different amino acids resulted in the discovery of a new class of hybrid compounds that targets both planktonic and biofilms bacteria in Staphylococcus aureus strains and are far more potent anti-biofilm agents than conventional antibiotics. Unlike dehydroabietic acid, these compounds can disrupt biofilms within a short time period and compromise the integrity of the bacterial membrane. Two of the compounds identified in our study are the most potent abietane-type anti-biofilm agents reported so far and display robust activity against pre-formed biofilms at concentrations only 3–6-fold higher than those required to inhibit biofilm formation. Their easy preparation based on proteolysis-resistant d- and unusual amino acids makes them useful chemical probes to gain a deeper understanding of bacterial biofilms and outstanding candidates for further development into new drugs to fight infections.
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Journal: European Journal of Medicinal Chemistry - Volume 102, 18 September 2015, Pages 68–79