Semisynthetic cephalosporins. III. Synthesis and structure activity relationships of novel orally active 7-[4-hydroxy-3-(substituted methyl)phenyl]-acetamido-3-cephem-4-carboxylic acids.
A family of novel optically active alpha-amino-3-substituted-methyl-4-hydroxy benzene acetic acids (3) have been prepared. A number of these amino acids were converted to a group of cephalosporins (12). Compound 12A showed the most interesting activity in vitro and in vivo, primarily against Gram-positive organisms and was shown to be well absorbed orally.
D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D007928:Lethal Dose 50; D051379:Mice; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D002511:Cephalosporins