| Literature DB >> 23755848 |
Matthew F Brown1, Mark J Mitton-Fry, Joel T Arcari, Rose Barham, Jeffrey Casavant, Brian S Gerstenberger, Seungil Han, Joel R Hardink, Thomas M Harris, Thuy Hoang, Michael D Huband, Manjinder S Lall, M Megan Lemmon, Chao Li, Jian Lin, Sandra P McCurdy, Eric McElroy, Craig McPherson, Eric S Marr, John P Mueller, Lisa Mullins, Antonia A Nikitenko, Mark C Noe, Joseph Penzien, Mark S Plummer, Brandon P Schuff, Veerabahu Shanmugasundaram, Jeremy T Starr, Jianmin Sun, Andrew Tomaras, Jennifer A Young, Richard P Zaniewski.
Abstract
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.Entities:
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Year: 2013 PMID： 23755848 DOI： 10.1021/jm400560z
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446