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ID: ALA1124257

Journal: J Med Chem

Title: An examination of O-2-isocephems as orally absorbable antibiotics.

Authors: Mastalerz H, Menard M, Vinet V, Desiderio J, Fung-Tomc J, Kessler R, Tsai Y.

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.

CiteXplore: 3373488

DOI: 10.1021/jm00401a020