Studies on beta-lactam antibiotics. XIII. Synthesis and structure-activity relationships of 7 beta-[(Z)-2-aryl-2-carboxymethoxyiminoacetamido]-3-vinylcepha losporins .
The synthesis, antibacterial activity and oral absorption of the 7 beta -[(Z)-2-aryl-2-carboxymethoxyiminoacetamido]-3- vinylcephalosporins are described. Of these cephalosporin derivatives, 7 beta-[(Z)-2-(2-amino-4-thiazolyl)-2-carboxymethoxyiminoacetamido]- 3-vinylcephalosporin exhibited the highest activity against Gram-negative bacteria and showed also good excretion after oral administration to rats. In addition, the effects on the antibacterial activity and oral absorption of the amino function on the thiazole ring are discussed.
Kawabata
K
K
Yamanaka
H
H
Takasugi
H
H
Takaya
T
T
D000042:Absorption; D000284:Administration, Oral; D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D014316:Tritium
D002511:Cephalosporins; D014316:Tritium