1984 Volume 32 Issue Supplement2 Pages 20-35
The in vitro antibacterial activities of TA-058, a new amoxicillin derivative with aspartic acid residue, were found to be broad against both gram positive and negative bacteria, especially effective against S. Pyogenes, S. pneumoniae and P. mirabilis. Its activities against S. aureus, S. faecalis, E. coli and B. fragilis were sufficient as PIPC, whereas less active against K pneumoniae, P. inconstans and P. aeruginosa. The minimum inhibitory concentrations of most of the strains of P. vulgaris and S. marcescens were distributed in over 100μg/ml.
TA-058 was stable in cepharosporinase but labile in penicillinase as those other broad spectrum penicillins.
Therapeutic effects of TA-058 in the experimentally infected mice either with E. coli C-11 or K. pneumoniae No10 or P. aeruginosa PI-21 were similar to those of PIPC and thus, superior to CBPC, SBPC, ABPC and AMPC but inferior to APPC. Therapeutic effects on cyclophosphamidetreated mice infected either with E. coli C-11 or P. aeruginosa PI-21 were superior to CBPC, PIPC, ABPC or CEZ.