STUDIES ON CEPHALOSPORIN ANTIBIOTICS

I. SYNTHESIS, ANTIBACTERIAL ACTIVITY AND ORAL ABSORPTION OF NEW 3-(O-SUBSTITUTED)-7β-[D-α-AMINO-α-(4-HYDROXYPHENYL)ACETAMIDO]CEPHALOSPORINS

Abstract

The synthesis, antibacterial activity and oral absorption of new 7β-[D-α-amino-α-(4-hydroxyphenyl)acetamido]cephalosporins (1) with various O-substituents at the C-3 position of a cephalosporin nucleus are described. Of these, the cephalosporins (1b-1e) having an alkoxycarbonylmethoxy group at the C-3 position showed good oral absorption in rats as well as potent activity against Gram-positive bacteria. The structure-activity relationships of 1 are also presented.