An examination of O-2-isocephems as orally absorbable antibiotics.
The synthesis and structure-activity relationships of a series of orally absorbed O-2-isocephems are described. These compounds possessed a D-[(p-hydroxyphenyl)glycyl]amino substituent at the 7-position while the substituent at the 3-position was varied. Relative to the analogous cephems, the O-2-isocephems exhibited comparable to better activity against Gram-positive organisms. Against Gram-negative organisms, their activity was variable but did indicate a lower beta-lactamase stability. Following oral administration, the O-2-isocephems generally exhibited longer half-lives but lower Cmax's and urinary recoveries.
Mastalerz
H
H
Bristol-Myers Pharmaceutical Group, Candiac, Quebec, Canada.
Menard
M
M
Vinet
V
V
Desiderio
J
J
Fung-Tomc
J
J
Kessler
R
R
Tsai
Y
Y
D000284:Administration, Oral; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D002511:Cephalosporins