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, , are reported along with the finding that is 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 binding to its target PBP3.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7590959 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.0c00255 | DOI Listing |
Publication Analysis
Top Keywords
multidrug-resistant gram-negative
8
γ-lactam siderophore
4
siderophore antibiotic
4
antibiotic effective
4
effective multidrug-resistant
4
gram-negative bacilli
4
bacilli treatment
4
treatment multidrug-resistant
4
gram-negative bacterial
4
bacterial pathogens
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!