Synthesis, biological evaluation and structure-activity relationships of 5-arylidene tetramic acids with antibacterial activity against methicillin-resistant Staphylococcus aureus

2020 ◽  
Vol 30 (10) ◽  
pp. 127107 ◽  
Author(s):  
Dimitris Matiadis ◽  
Dimitrios Tsironis ◽  
Valentina Stefanou ◽  
Spyridon Boussias ◽  
Angeliki Panagiotopoulou ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Biological Evaluation ◽  
Methicillin Resistant ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Tetramic Acids

scholarly journals Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents

2019 ◽  
Vol 15 ◽  
pp. 1468-1474
Author(s):  
Leticia Monjas ◽  
Peter Fodran ◽  
Johanna Kollback ◽  
Carlo Cassani ◽  
Thomas Olsson ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Natural Product ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Methicillin Resistant ◽  
Structure Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Novel Antibiotics

The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure–activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant Staphylococcus aureus (MRSA).

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