Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity
Journal of Medicinal Chemistry
Herein we describe the structure-aided design and synthesis of a series of pyridone-conjugated monobactam analogues with in vitro antibacterial activity against clinically relevant Gram-negative species including Pseudomonas aeruginosa, Klebsiella pneumoniae, and Escherichia coli. Rat pharmacokinetic studies with compound 17 demonstrate low clearance and low plasma protein binding. In addition, evidence is provided for a number of analogues suggesting that the siderophore receptors PiuA and PirA play a role in drug uptake in P. aeruginosa strain PAO1.
Mitton-Fry, Mark; Brown, Matthew; and Arcari, Joel, "Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity" (2013). Chemistry Faculty Work. 7.
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