Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus
ACS Medicinal Chemistry Letters2012Vol. 3(8), pp. 626–630
Citations Over TimeTop 16% of 2012 papers
Tihomir Tomašič, Roman Šink, Nace Zidar, Anja Fic, Carlos Contreras‐Martel, Andréa Dessen, Delphine Patin, Didier Blanot, Manica Müller‐Premru, Stanislav Gobec, Anamarija Zega, D. Kikelj, Lucíja Peterlin Mašič
Abstract
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.
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