Studies on cephalosporin antibiotics. I. Synthesis, antibacterial activity and oral absorption of new 3-(O-substituted)-7 beta-[D-alpha-amino-alpha-(4-hydroxyphenyl)acetamido]cephalosporins.
The synthesis, antibacterial activity and oral absorption of new 7 beta-[D-alpha-amino-alpha-(4-hydroxyphenyl)acetamido]cephalosporins (1) with various O-substituents at the C-3 position of a cephalosporin nucleus are described. Of these, the cephalosporins (1b-1e) having an alkoxycarbonylmethoxy group at the C-3 position showed good oral absorption in rats as well as potent activity against Gram-positive bacteria. The structure-activity relationships of 1 are also presented.
Yokoo
C
C
Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.
Goi
M
M
Onodera
A
A
Murata
M
M
Nagate
T
T
Watanabe
Y
Y
Sota
K
K
D000284:Administration, Oral; D000818:Animals; D002511:Cephalosporins / Q000096:biosynthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D007408:Intestinal Absorption; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008826:Microbial Sensitivity Tests; D051381:Rats; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D002511:Cephalosporins