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Succinic Acids as Potent Inhibitors of Plasmid-borne IMP-1 Metallo-β-lactamase*
TLDR
Determination of high resolution crystal structures and molecular modeling of succinic acid inhibitor complexes with IMP-1 has allowed an understanding of the potency, stereochemistry, and structure-activity relationships of these inhibitors. Expand
In Vitro Activities of the Potent, Broad-Spectrum Carbapenem MK-0826 (L-749,345) against Broad-Spectrum β-Lactamase-and Extended-Spectrum β-Lactamase-Producing Klebsiella pneumoniae and Escherichia
ABSTRACT An important mechanism of bacterial resistance to β-lactam antibiotics is inactivation by β-lactam-hydrolyzing enzymes (β-lactamases). The evolution of the extended-spectrum β-lactamasesExpand
Antibiotic sensitization using biphenyl tetrazoles as potent inhibitors of Bacteroides fragilis metallo-beta-lactamase.
TLDR
BPT inhibitors can sensitize a resistant B. fragilis clinical isolate expressing metallo-beta-lactamase to the antibiotics imipenem or penicillin G but not to rifampicin. Expand
Inhibition of IMP-1 metallo-beta-lactamase and sensitization of IMP-1-producing bacteria by thioester derivatives.
TLDR
Thioester IMP-1 inhibitors offer an encouraging start to overcoming metallo-beta-lactamase-mediated resistance in bacteria. Expand
Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.
TLDR
This class of compounds showed enhanced water solubility while maintaining potent activity against MRS and introduction of a 1-beta-methyl substituent was found to improve pharmacokinetics. Expand
Soluble penicillin-binding protein 2a: beta-lactam binding and inhibition by non-beta-lactams using a 96-well format.
TLDR
A 96-well-filter binding assay using recombinant, soluble PBP2a which allows for kinetic measurement of penicillin binding is described and several non-beta-lactam inhibitors including Cibacron blue have been found which exhibit IC50 values between 10 and 30 microM. Expand
Structure-activity relationships of biphenyl tetrazoles as metallo-β-lactamase inhibitors
Resistance to carbapenem antibiotics in Gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-β-lactamase, which renders the drug inactive. Biphenyl tetrazoles containingExpand
Synthesis and SAR of thioester and thiol inhibitors of IMP-1 Metallo-β-Lactamase
Potent thioester and thiol inhibitors of IMP-1 metallo-β-lactamase have been synthesized employing a solid-phase Mitsunobu reaction as the key step.
Synthesis and properties of 2-(naphthosultamyl)methyl-carbapenems with potent anti-MRSA activity: discovery of L-786,392.
TLDR
Based on a combination of excellent in vitro antibacterial activity, acceptable mouse acute toxicity, and a desirable fragmentation pattern on beta-lactam ring opening, the analog 2g (L-786,392) was selected for extended evaluation. Expand
Benzothiazolylthio carbapenems: potent anti-MRSA agents
Abstract A series of sulfur-linked benzothiazolyl carbapenems has been prepared and evaluated against a battery of microorganisms. Many of the compounds displayed good activity againstExpand
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