In Vitro Antibacterial Activity of LJC 11,036, an Active Metabolite of L-084, a New Oral Carbapenem Antibiotic with Potent Antipneumococcal Activity

Autor: Muneo Hikida, Toshiharu Shiba, Atsumi Igarashi, Masataka Kitamura, Kouju Itahashi
Rok vydání: 1999
Předmět:
Dipeptidases
Ofloxacin
Imipenem
Lactams
Klebsiella pneumoniae
Levofloxacin
Microbial Sensitivity Tests
Muramoylpentapeptide Carboxypeptidase
Biology
beta-Lactams
medicine.disease_cause
beta-Lactamases
Microbiology
Haemophilus influenzae
chemistry.chemical_compound
Minimum inhibitory concentration
Anti-Infective Agents
Bacterial Proteins
Drug Stability
Streptococcus pneumoniae
medicine
Penicillin-Binding Proteins
Pharmacology (medical)
Antibacterial agent
Pharmacology
Cefdinir
Minimum bactericidal concentration
Escherichia coli Proteins
Faropenem
biology.organism_classification
Serine-Type D-Ala-D-Ala Carboxypeptidase
Anti-Bacterial Agents
Cephalosporins
Infectious Diseases
Carbapenems
Hexosyltransferases
chemistry
Susceptibility
Peptidyl Transferases
Thienamycins
Peptidoglycan Glycosyltransferase
Carrier Proteins
Protein Binding
medicine.drug
Zdroj: Antimicrobial Agents and Chemotherapy. 43:2010-2016
ISSN: 1098-6596
0066-4804
Popis: LJC 11,036 is the active metabolite of L-084, a novel oral carbapenem that exhibits potent broad-spectrum activity. Antibacterial activities of LJC 11,036 against clinical isolates from respiratory infections, such as Streptococcus pneumoniae ( n = 52), Streptococcus pyogenes ( n = 19), Haemophilus influenzae ( n = 50), Klebsiella pneumoniae ( n = 53), and Moraxella catarrhalis ( n = 53), and from urinary-tract infections, such as Escherichia coli ( n = 53) (MICs at which 90% of the isolates were inhibited [MIC 90 s], 0.1, ≤0.006, 0.39, 0.05, 0.05, and 0.05 μg/ml, respectively), were 2- to 64-fold higher than those of imipenem, cefdinir, and faropenem. Moreover, against these bacterial species, except for H. influenzae , the MIC 90 s of LJC 11,036 were 4- to 512-fold lower than those of levofloxacin. LJC 11,036 showed bactericidal activity equal or superior to that of imipenem. Bactericidal activity against penicillin-resistant S. pneumoniae (PRSP) did not vary with the phase of growth. LJC 11,036 had potent activity against various β-lactamase-producing strains, excluding carbapenemase producers. Against renal dehydropeptidase-I, LJC 11,036 was more stable than imipenem. Furthermore, LJC 11,036 produced in vitro postantibiotic sub-MIC effects against PRSP HSC-3 (6.0 h at one-fourth the MIC) and H. influenzae LJ5 (9.2 h at one-half the MIC). LJC 11,036 showed high binding affinities for PBP1A, -1B, -2A/2X, -2B, and -3 of PRSP and for PBP1B, -2, -3A, and -3B of H. influenzae .
Databáze: OpenAIRE
Externí odkaz: