Lactol esters of ampicillin.

Syntheses and hydrolysis of basic and dibasic ampicillin esters tailored for intracellular accumulation.

Readily hydrolysable basic and dibasic esters of ampicillin were synthesised by alkylation of the carboxylate function of ampicillin to obtain prodrugs that may accumulate in cells and allow for an intracellular delivery of ampicillian (Fan et al., Bioorg. Med. Chem. Lett. 1997, 7, 3107). We found that the beta-lactam ring cleavage and the hydrolysis of the ester function were competitive react...

Bioavailability of ampicillin (anhydrous) and ampicillin trihydrate.

Ampicillin susceptibility and ampicillin-induced killing rate of Escherichia coli.

The killing rate induced by ampicillin was determined in 20 strains of Escherichia coli. The apparent generation rate constant for each E. coli showed a characteristic concentration-dependent course. This course can be mathematically described and is determined by four parameters. Three of these parameters determine the speed of the process, and the fourth parameter determines a minimal concent...

Effects of ampicillin-amikacin and ampicillin-rifampin on enterococci.

Fifty-seven clinical isolates of enterococcus were tested for susceptibility to 10 antibiotics in a microtiter broth dilution system. Amoxicillin, ampicillin, vancomycin, and rifampin inhibited all strains at concentrations easily achievable in blood. Resistance to rifampin developed rapidly. Of the aminoglycosides, gentamicin was most active, followed in decreasing order by tobramycin, amikaci...

Ampicillin Treatment of Typhoid Carriers.

THE change in the clinical course of typhoid fever due to treatment with chloramphenicol has been one of the more dramatic triumphs of the antibiotic age. A prolonged fever has been converted into a short sharp febrile illness, so that the patient suffering from the disease, instead of being dangerously ill for several weeks, may well be sitting up in bed after three or four days on chloramphen...