In vitro and in vivo antibacterial activities of ME1220 and ME1221, novel cephalosporins.
The antibacterial activities and serum pharmacokinetic properties of ME1220 and ME1221, new aminothiazolylalkoxyiminoacetylcephalosporins having an N-alkylpyridiniumthiomethyl side chain at C-3, were compared with those of cefpirome and ceftazidime. ME1220 and ME1221 exhibited broad antibacterial activity against Gram-positive and Gram-negative bacteria. The in vitro and in vivo activities of ME1220 were similar to cefpirome, while ME1221 was superior to ceftazidime against almost all test organisms except pseudomonas. On intravenous injection in rats, ME1220 and ME1221 were excreted mainly in the urine. ME1221 was excreted moderately in the bile and showed higher serum concentration and AUC than those of ME1220.
Okamoto
R
R
Episome Institute, Gunma, Japan.
Tamura
A
A
Yoshida
T
T
Komiya
I
I
Ogino
H
H
Inouye
S
S
Kondo
S
S
Inoue
M
M
Mitsuhashi
S
S
D000818:Animals; D002442:Ceftazidime / Q000493:pharmacokinetics / Q000494:pharmacology; D002511:Cephalosporins / Q000493:pharmacokinetics / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D051381:Rats; D011919:Rats, Inbred Strains; D001618:beta-Lactamases / Q000378:metabolism; D000097572:Cefpirome
D002442:Ceftazidime; D002511:Cephalosporins; D001618:beta-Lactamases; D000097572:Cefpirome; C073232:ME 1221; C073231:ME 1220