Semisynthetic penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains. Synthesis and structure-activity relationships.
A series of penicillins and cephalosporins containing the substituted 6-vinyl-1,2-dihydro-2-oxo- and 1,4-dihydro-4-oxo-3-pyridinecarboxylic acid side chains has been prepared and compared to piperacillin and cefoperazone. The compounds show good activity when tested in vitro against an array of Gram-negative bacteria. In vitro activity was also demonstrated against several species of Gram-positive bacteria. Two compounds, 14 and 21, show good in vivo activity when tested against Klebsiella pneumoniae, Enterobacter cloacae, and two strains of Pseudomonas aeruginosa.
D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001424:Bacterial Infections / Q000188:drug therapy; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D051379:Mice; D010406:Penicillins / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002511:Cephalosporins; D010406:Penicillins