ANTIBACTERIAL ACTIVITY OF SERUM AFTER ORAL DOSES OF TRIACETYLOLEANDOMYCIN, ERYTHROMYCIN, POTASSIUM PENICILLIN V AND PENICILLIN V

PEDIATRICS ◽  
1958 ◽  
Vol 22 (3) ◽  
pp. 422-431
Author(s):  
Calvin M. Kunin ◽  
Charles V. Pryles ◽  
Maxwell Finland

Triacetyloleandomycin, in this study, produced antistreptococcal and antistaphylococcal activity in the serum of normal men and in children comparable to that produced by equivalent amounts of the erythromycin preparations used. The better and more rapid absorption of oral doses of potassium penicillin V as compared with acid penicillin V was confirmed. It was also shown that penicillin V, either as the acid or as the potassium salt, produced significantly higher peak levels of antibacterial activity than either erythromycin or triacetyloleandomycin.

2017 ◽  
Vol 95 (9) ◽  
pp. 927-934 ◽  
Author(s):  
Elena Fuentes-Paniagua ◽  
José M. Hernández-Ros ◽  
Juan Soliveri ◽  
José L. Copa-Patiño ◽  
Rafael Gómez ◽  
...  

Strategies to synthesize a cationic carbosilane dendron containing the antibiotic penicillin V potassium salt (PenVK) at the focal point are discussed. The preparation of such a compound requires the use of systems with no donor atoms such as N or S in their framework, because their presence favours the rupture of the penicillin β-lactam ring. The antibacterial activity of the new dendron containing ammonium groups, at the periphery, and the PenV moiety, at the focal point, against gram-positive Staphylococcus aureus strains was evaluated. These results were compared with those obtained for free PenVK, a related cationic dendron without a penicillin moiety at the focal point, and also compared with an equimolar mixture of this last dendron with free PenV. The data obtained indicate that, on one hand, the conjugation or interaction of PenV with cationic dendrons reduces its activity in comparison with free PenVK. On the other hand, the penicillin dendron is able to release the antibiotic in the presence of esterease, due to the breaking of the ester bond in this derivative.


1959 ◽  
Vol 260 (9) ◽  
pp. 408-412 ◽  
Author(s):  
Hans A. Hirsch ◽  
Calvin M. Kunin ◽  
Maxwell Finland ◽  
Clare Wilcox ◽  
Ann Najarian

PEDIATRICS ◽  
1963 ◽  
Vol 31 (1) ◽  
pp. 22-28
Author(s):  
Maxwell Stillerman ◽  
Stanley H. Bernstein ◽  
Martha Smith ◽  
Jack D. Gorvoy

The relative effectiveness of erythromycin propionate and K penicillin V in two dosage schedules was evaluated in the treatment of 261 cases of acute pharyngitis from which Group A hemolytic streptococci were recovered from December, 1958, to June, 1959. Erythromycin propionate, in a daily dose of 30 mg/kg up to 1.0 gm, and K penicillin V, in daily doses of 375 mg and 750 mg, were administered orally for 10 days. The adjusted bacterial cure rate was 78% among 86 patients treated with erythromycin, 72% among 102 patients treated with K penicillin V, 375 mg, and 88% among 73 patients treated with K penicillin V, 750 mg. The data indicate that K penicillin V was more effective in eradicating Group A streptococci from the pharynx in a daily dose of 750 mg than 375 mg, and suggest that erythromycin propionate in the dosage used, was less effective than K penicillin V, 750 mg, but equally as effective as K penicillin V, 375 mg daily. The incidence, time of occurrence, and results of retreatments of bacterial relapses are presented, and two possible causes of relapses are considered.


PEDIATRICS ◽  
1963 ◽  
Vol 32 (5) ◽  
pp. 919-922
Author(s):  
F. WHITEHOUSE ◽  
S. A. OBENG ◽  
A. R. PEQUET ◽  
J. K. CHAMNESS ◽  
J. K. JENDER ◽  
...  

A single dose of 200-400,000 units of oral potassium penicillin V is absorbed rapidly in fasting febrile children and infants to produce high serum levels. These levels are similar to those of afebrile children in the same age groups. From this standpoint, therapy of acutely ill febrile children with oral potassium penicillin V in reliable when penicillin is indicated.


2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Pablo E. Romo ◽  
Braulio Insuasty ◽  
Rodrigo Abonia ◽  
María del Pilar Crespo ◽  
Jairo Quiroga

A versatile method for the synthesis of new oxindoles was developed by the reaction between substituted isatins and 5-aminopyrazoles. The reaction was carried out at room temperature in ethanol using p-toluenesulfonic acid as the catalyst. The products were obtained with acceptable to excellent yields (44–96%). Structures of the new compounds were unambiguously established by spectroscopic and analytical techniques. The antibacterial activity was determined by microdilution assays. Compounds 3b, 3e, and 3g showed antistaphylococcal activity, particularly compound 3e displayed a potent activity against the vancomycin intermediate Staphylococcus aureus (VISA). Compounds 3i, 3j, and 3o inhibited Neisseria gonorrhoeae growth.


2007 ◽  
Vol 51 (4) ◽  
pp. 1559-1562 ◽  
Author(s):  
Aldona L. Baltch ◽  
William J. Ritz ◽  
Lawrence H. Bopp ◽  
Phyllis B. Michelsen ◽  
Raymond P. Smith

ABSTRACT We investigated the antistaphylococcal activity of daptomycin, vancomycin, oxacillin, gentamicin, and rifampin in human monocyte-derived macrophages. Compared with vancomycin and oxacillin, daptomycin had the most rapid and greatest antibacterial activity, but that of oxacillin was most sustained. The combination of daptomycin, gentamicin, and rifampin was most effective intracellularly, while daptomycin plus gentamicin and the three-drug combination were most effective extracellularly, completely eliminating viable Staphylococcus aureus.


1962 ◽  
Vol 3 (3) ◽  
pp. 284-304 ◽  
Author(s):  
Jack S. Remington ◽  
Maxwell Finland ◽  
Charles W. Dunnett ◽  
R. R. Roepke ◽  
Clare Wilcox ◽  
...  

1998 ◽  
Vol 42 (6) ◽  
pp. 1447-1453 ◽  
Author(s):  
Joy L. Silen ◽  
Amy T. Lu ◽  
Dennis W. Solas ◽  
Medini A. Gore ◽  
Derek Maclean ◽  
...  

ABSTRACT A sensitive lawn-based format has been developed to screen bead-tethered combinatorial chemical libraries for antimicrobial activity. This method has been validated with beads linked to penicillin V via a photocleavable chemical linker in several analyses including a spike-and-recover experiment. The lawn-based screen sensitivity was modified to detect antibacterial compounds of modest potency, and a demonstration experiment with a naive combinatorial library of over 46,000 individual triazines was evaluated for antibacterial activity. Numerous hits were identified, and both active and inactive compounds were resynthesized and confirmed in traditional broth assays. This demonstration experiment suggests that novel antimicrobial compounds can be easily identified from very large combinatorial libraries of small, nonpeptidic compounds.


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