title: An examination of O-2-isocephems as orally absorbable antibiotics.
abstract: 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.
authors: Bristol-Myers Pharmaceutical Group, Candiac, Quebec, Canada.
authors: H
authors: H
authors: Mastalerz
authors: M
authors: M
authors: Menard
authors: V
authors: V
authors: Vinet
authors: J
authors: J
authors: Desiderio
authors: J
authors: J
authors: Fung-Tomc
authors: R
authors: R
authors: Kessler
authors: Y
authors: Y
authors: Tsai
mesh_terms: D000284:Administration, Oral; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D002511:Cephalosporins