A new parenteral cephalosporin. SK&F 59962: 7 trifluoromethylthioacetamido 3 (1 methyl 1H tetrazol 5 ylthiomethyl) 3 cephem 4 carboxylic acid. Chemistry and structure activity relationships

Article abstract of DOI:10.7164/antibiotics.28.463

The synthesis, microbiological profile and in vivo effectiveness in laboratory animals of a series of cephalosporins having 7 acyl substituents derived from methylthioacetic acid are described. Structure activity relationships examined include the effect of oxidation of the side chain sulfur atom, replacement of the (side chain) methyl hydrogens by fluorine and replacement of the 3 acetoxy substituent by thioheterocycles. One derivative, 7 trifluoromethylthioacetamido 3 (1 methyl 1H tetrazol 5 ylthiomethyl) 3 cephem 4 carboxylic acid (SK and F 59962), was found to have outstanding antibacterial activity in vitro and in vivo.