A new aminothiazolylcephalosporin having 1-carboxyethoxyimino group, ME1228.
Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities. Among these cephalosporins, ME1228 having (S)-1-carboxyethoxyimino substituent and being combined with an (N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.
Shibahara
S
S
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
Okonogi
T
T
Yoshida
T
T
Murai
Y
Y
Kudo
T
T
Inouye
S
S
Kondo
S
S
D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D002511:Cephalosporins / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D055598:Chemical Phenomena; D002621:Chemistry; D004927:Escherichia coli Infections / Q000188:drug therapy; D007536:Isomerism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011552:Pseudomonas Infections / Q000188:drug therapy
D002511:Cephalosporins; C061366:ME 1228