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A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli
- Source :
- Journal of Medicinal Chemistry; June 2020, Vol. 63 Issue: 11 p5990-6002, 13p
- Publication Year :
- 2020
-
Abstract
- Treatment of multidrug-resistant Gram-negative bacterial pathogens represents a critical clinical need. Here, we report a novel γ-lactam pyrazolidinone that targets penicillin-binding proteins (PBPs) and incorporates a siderophore moiety to facilitate uptake into the periplasm. The MIC values of γ-lactam YU253434, 1, are reported along with the finding that 1is resistant to hydrolysis by all four classes of β-lactamases. The druglike characteristics and mouse PK data are described along with the X-ray crystal structure of 1binding to its target PBP3.
Details
- Language :
- English
- ISSN :
- 00222623 and 15204804
- Volume :
- 63
- Issue :
- 11
- Database :
- Supplemental Index
- Journal :
- Journal of Medicinal Chemistry
- Publication Type :
- Periodical
- Accession number :
- ejs53261097
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.0c00255