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  • Title: 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.
    Author: DeJohn D, Domagala JM, Haskell TH, Heifetz CL, Huang GG, Kaltenbronn JS, Krolls U.
    Journal: J Antibiot (Tokyo); 1985 Mar; 38(3):372-9. PubMed ID: 4008330.
    Abstract:
    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.
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