Studies on cephalosporin antibiotics. I. Synthesis, antibacterial activity and oral absorption of new 3- (O-substituted) -7.Beta.- (D-.Alpha.-amino-.Alpha.- (4-hydroxyphenyl) acetamido) cephalosporins

Yokoo, C.; Goi, M.; Onodera, A.; Murata, M.; Nagate, T.; Watanabe, Y.; Sota, K.

The Journal of Antibiotics 41(2): 170-180


DOI: 10.7164/antibiotics.41.170
Accession: 068516274

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The synthesis, antibacterial activity and oral absorption of new 7 beta-[D-alpha-amino-alpha-(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.