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, 3...

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Bibliographic Details
Published in:	Journal of antibiotics Vol. 43; no. 9; p. 1150
Main Authors:	Katano, K, Ogino, H, Iwamatsu, K, Nakabayashi, S, Yoshida, T, Komiya, I, Tsuruoka, T, Inouye, S, Kondo, S
Format:	Journal Article
Language:	English
Published:	Japan 1990
Subjects:	Animals Bacteria - drug effects Bacterial Infections - drug therapy Cephalosporins - chemical synthesis Cephalosporins - pharmacology Cephalosporins - therapeutic use Magnetic Resonance Spectroscopy Male Mice Mice, Inbred ICR Rats Structure-Activity Relationship
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Summary:	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.
ISSN:	0021-8820
DOI:	10.7164/antibiotics.43.1150