IN VITRO AND IN VIVO ANTIBACTERIAL PROPERTIES OF T-2588, A NEW ORAL CEPHEM ANTIBIOTIC

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T-2588 is a new orally absorbable prodrug of T-2525. In vitro and in vivo antibacterial activity of T-2588 and T-2525 was examined and the following results were obtained. 1) T-2525 had a broad antibacterial spectrum against gram-positive and gram-negative bacteria, including resistant ones to the other cephem antibiotics, and showed the potent antibacterial activity, especially against Streptococcus pyogenes, S. pneumoniae, Citrobacter sp., Enterobacter sp., Indole (+) Proteus sp., Serratia marcescens, Haemophilus influenzae and Bacteroides fragilis. 2) The antibacterial activity of T-2525 was hardly changed by pH of medium and the kind of medium, and the addition of human serum into culture media. However, the antibacterial activity of T-2525 against several bacterial species and strains tended to decrease slightly with the increase of inoculum size. 3) The antibacterial activity of T-2525 was bactericidal at MIC. 4) T-2525 was very stable to penicillinase and cephalosporinase. 5) The affinity of T-2525 for penicillin binding proteins of E. coli was stronger in the following order, PBP 3>1Bs>1A. 6) The therapeutic effects of T-2588 in mice infected with gram-negative bacteria were superior to those of reference compounds, while they were inferior to those of reference compounds against infection with Staphylococcus aureus.
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