1384338-83-3Relevant academic research and scientific papers
Dual inhibitor of MurD and MurE ligases from escherichia coli and staphylococcus aureus
Tomasic, Tihomir,Sink, Roman,Zidar, Nace,Fic, Anja,Gobec, Stanislav,Zega, Anamarija,Kikelj, Danijel,Masic, Lucija Peterlin,Contreras-Martel, Carlos,Dessen, Andrea,Patin, Delphine,Blanot, Didier,Mueller-Premru, Manica
, p. 626 - 630,5 (2020/08/31)
MurD and MurE ligases, consecutive enzymes participating in the intracellular steps of bacterial peptidoglycan biosynthesis, are important targets for antibacterial drug discovery. We have designed, synthesized, and evaluated the first d-glutamic acid-containing dual inhibitor of MurD and MurE ligases from Escherichia coli and Staphylococcus aureus (IC50 values between 6.4 and 180 μM) possessing antibacterial activity against Gram-positive S. aureus and its methicillin-resistant strain (MRSA) with minimal inhibitory concentration (MIC) values of 8 μg/mL. The inhibitor was also found to be noncytotoxic for human HepG2 cells at concentrations below 200 μM.
