STUDIES ON β-LACTAM ANTIBIOTICS: XIX. STRUCTURE-ACTIVITY RELATIONSHIPS OF CEPHALOSPORINS HAVING A THIADIAZOLYLTHIOMETHYL GROUP AT THE C-3 SIDE CHAIN

The synthesis and antibacterial activity of 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-(hydroxy or alkoxy)iminoacetamido] cephalosporins with various thiadiazolylthiomethyl moieties at the 3-position are discussed. Of the compounds (1a-1e, 7a-7d), 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-hydroxyiminoacetamido]-3-[(...

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Veröffentlicht in:	Journal of antibiotics 1991/05/25, Vol.44(5), pp.507-516
Hauptverfasser:	INAMOTO, YOSHIKO, GOTO, JIRO, SAKANE, KAZUO, KAMIMURA, TOSHIAKI, TAKAYA, TAKAO
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Ceftizoxime - analogs & derivatives Ceftizoxime - pharmacology Cephalosporins - chemical synthesis Cephalosporins - pharmacology Medical sciences Microbial Sensitivity Tests Pharmacology. Drug treatments Staphylococcus aureus - drug effects Structure-Activity Relationship
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Zusammenfassung:	The synthesis and antibacterial activity of 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-(hydroxy or alkoxy)iminoacetamido] cephalosporins with various thiadiazolylthiomethyl moieties at the 3-position are discussed. Of the compounds (1a-1e, 7a-7d), 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-hydroxyiminoacetamido]-3-[(1, 2, 4-thiadiazol-5-yl)thiomethyl]cephalosporin (1d: FK312) exhibited the highest activity against Gram-positive and Gram-negative bacteria, especially, against methicillin-resistant Staphylococcus aureus. Furthermore, the pharmacokinetic profiles of the compound 1d showed longer serum levels than that of ceftriaxone in rats.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.44.507