The expression of penicillin binding protein 2a (PBP2a) is the basis for the broad clinical resistance to the β-lactam antibiotics by methicillin-resistant Staphylococcus aureus (MRSA). The high-molecular mass penicillin binding proteins of bacteria catalyze in separate domains the transglycosylase and transpeptidase activities required for the biosynthesis of the peptidoglycan polymer that com...

The time course of EPSCs and IPSCs is at least partly determined by the concentration profile of neurotransmitter acting on postsynaptic receptors. Several recent reports have suggested that the peak synaptic cleft concentration of the inhibitory neurotransmitter GABA likely reaches at least 500 microM, a level that saturates the GABAA receptor. In the course of investigating the experimental a...

Against most test strains of Gram-negative bacilli, the in vitro effect of FR-31564 together with beta-lactam antibiotics or trimethoprim was strongly synergistic; with tetracycline and nalidixic acid the effect was additive; and with gentamicin and sulfamethoxazole the effect was additive or antagonistic. FR-31564 was markedly synergistic with beta-lactam antibiotics against beta-lactam antibi...

Fifty-four milk samples from commercial sources that tested positive for beta-lactam antibiotics were analyzed by a multiresidue liquid chromatographic (LC) procedure based on LC fractionation. Penicillin G and cephapirin were the beta-lactam antibiotics found most frequently. Some samples did not contain detectable beta-lactam antibiotics. In a few, the presence of a beta-lactam antibiotic was...

β-Lactam peptides were envisioned as conformational constraints in antigenic peptides (APs). Three different β-lactam tripeptides of varying flexibility were prepared in solution and incorporated in place of the central part of the altered melanoma associated antigenic peptide Leu(27)-Melan-A(26-35) using solid phase synthesis techniques. Upon TFA cleavage from the solid support, an unexpected ...

There have been conflicting data about the interactions between vancomycin and beta-lactam agents against Staphylococcus aureus strains with heterogeneous resistance to vancomycin. We evaluated the efficacy of these combinations against Mu 3 and heterogeneously vancomycin-resistant S. aureus (hetero-VRSA) strains which were isolated from Korean patients using a population analysis method. Antag...

The inhibition effect of several beta-lactam antibiotics on the uptake of [14C]benzylpenicillin (PCG) into isolated rat hepatocytes was studied. Monobasic beta-lactam antibiotics such as apalcillin, cloxacillin, nafcillin, piperacillin, cefmetazole, cefoperazone, cefpiramide and cephalothin significantly inhibited the uptake of PCG, while amphoteric beta-lactam antibiotics such as amoxicillin, ...

The synthesis of cis-N-[a-carbobenzyloxy-b-(p-hydroxyphenyl)ethyl]-3-phthalimido-4-styryl-2-azetidinone is described. We have found that the electron-rich Schiff bases can afford the cis-b-lactam ring even in the presence of the free hydroxyl functions. The mechanisms of cis and trans-b-lactam ring formation are discuss...

Significant advances have been made in the structure-based engineering of enzymes useful for beta-lactam antibiotic production. Structure-based engineering of penicillin G acylase and cephalosporin acylase has resulted in improved enzymes for use in enzymatic production processes. The structures of many other enzymes that could be used in the production of beta-lactam antibiotics, such as enzym...