New Carbapenem Antibiotics Iv. Inhibitory Activity against /3-lactamases
نویسندگان
چکیده
New carbapenern antibiotics, C-19393 S2 and H2, have been found to be potent and broadspectrum inhibitors of /3-lactamases. Among 11 types of /3-lactamases tested, those from Escherichia coli (plasmid-bearing), Klebsiella pneumoniae, Proteus vulgaris, Serratia marcescens and Bacteroides fragilis were especially sensitive. They also inhibited cephalosporinases insensitive to clavulanic acid. The inhibition by C-19393 S2 and H2 was of progressive type, except for the inhibition of E. coli enzyme (plasmid-mediated type I) by C-19393 H2. The inhibition of E. coli jS-lactamase by C-19393 S2 was irreversible, while that by C-19393 H2 was reversible.
منابع مشابه
Cephabacins, new cephem antibiotics of bacterial origin. IV. Antibacterial activities, stability to beta-lactamases and mode of action.
Cephabacin F group antibiotics with a 7-formylamino substituent showed antibacterial activity against a wide variety of bacteria including beta-lactamase-producing clinical isolates and anaerobic bacteria. Cephabacin H group antibiotics without the substituent showed more potent activity against Gram-positive bacteria than cephabacin F group antibiotics, but were not active against Gram-negativ...
متن کاملAntibacterial and Antibiofilm Activity of Grape Seed Extract Against Carbapenem Resistant and Biofilm Producer Enterobacteriaceae
Background and objectives: Carbapenem-resistant and biofilm producing Enterobacteriaceaeare a major health problem. This study was carried to determine the antibacterial and antibiofilm activity of grape seed extract (GSE) against carbapenem-resistant and biofilm producing Enterobacteriaceae isolates. Methods: Antibiotics susceptibility pattern...
متن کاملRapid spread of carbapenem-resistant Klebsiella pneumoniae in New York City: a new threat to our antibiotic armamentarium.
BACKGROUND Carbapenem antibiotics are used to treat serious infections caused by extended-spectrum beta-lactamase-carrying pathogens. Carbapenem resistance has been unusual in isolates of Klebsiella pneumoniae. In this study, the prevalence and molecular epidemiologic characteristics of carbapenem-resistant K pneumoniae are analyzed, and the experience involving 2 hospital outbreaks is describe...
متن کاملIn Vitro Activity of LK-157, a Novel Tricyclic Carbapenem As Broad-Spectrum -Lactamase Inhibitor
LK-157 is a novel tricyclic carbapenem with potent activity against class A and class C -lactamases. When tested against the purified TEM-1 and SHV-1 enzymes, LK-157 exhibited 50% inhibitory concentrations (IC50s) in the ranges of the clavulanic acid and tazobactam IC50s (55 nM and 151 nM, respectively). Moreover, LK-157 significantly inhibited AmpC -lactamase (IC50, 62 nM), as LK-157 was >2,00...
متن کاملAmino Acid Sequence Requirements at Residues 69 and 238 for the SME-1 -Lactamase To Confer Resistance to -Lactam Antibiotics
Carbapenem antibiotics have been used to counteract resistant strains of bacteria harboring -lactamases and extended-spectrum -lactamases. Four enzymes from the class A group of -lactamases, NMC-A, IMI-1, SME-1, and KPC-1, efficiently hydrolyze carbapenem antibiotics. Sequence comparisons and structural information indicate that cysteines at amino acid residues 69 and 238, which are conserved i...
متن کامل