An examination of O-2-isocephems as orally absorbable antibiotics

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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 substituents at the 7-position while the substituents 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 in mice.