Abstract
The synthesis of the orally absorbed 3-ethynylcephalosporin (1b) is described. In addition, the structure-activity relationships and oral absorption in rats of 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-carboxymethoxyiminoacetamido]cephalosporins (1) having various aliphatic hydrocarbon groups at the 3-position are discussed. Of these cephalosporins (1), 3-ethynylcephalosporin (1b) exhibited better activity against Staphylococcus aureus than the other cephalosporins (1a, 1c and 1d) and showed moderate oral absorption in rats.
