An Examination of O-2-Isocephems as Orally Absorbable Antibiotics

Article abstract of DOI:10.1021/jm00401a020

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 β-lactamase stability.Following oral administration, the O-2-isocephems generally exhibited longer half-lives but lower C_max's and urinary recoveries.