Synthesis and biological activity of (cyclopentenopyridinium) thiomethylcephalosporins.
Substituted (cyclopentenopyridinium)thiomethyl groups were introduced as C-3 substituents of (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-oxyimino]acetami docephalosporins. Structure-activity relationships of this class of cephalosporins are discussed on the basis of their MIC. The selected compounds, 3a and 4a (ME1221), having an acidic substituent, showed excellent in vivo efficacy and low toxicity.
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
K
K
Katano
H
H
Ogino
K
K
Iwamatsu
S
S
Nakabayashi
T
T
Yoshida
I
I
Komiya
T
T
Tsuruoka
S
S
Inouye
S
S
Kondo
D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D051381:Rats; D013329:Structure-Activity Relationship
D002511:Cephalosporins