THE FORMATION OF METABOLITES FROM CEPHALOSPORIN COMPOUNDS

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Abstract
Phenylacetyl cephalosporin gave rise to a further microbiologically active material in the urine of mice receiving the compound subcutaneously. This also occurred with cephalosporin C and its N-dinitrophenyl derivative. Many tissues, notably liver and kidney, are able to produce these compounds in vitro. The metabolites have less microbiological activity than their corresponding parent compounds. The metabolites are produced by deacetylation of the parent cephalosporins; different animal species have the ability to deacetylate different cephalosporins to different extents, e.g. man and monkey can deacetylate phenylacetyl cephalosporin but not cepahlosporin C. It is deduced that the clinical effectiveness of any cephalosporin will depend, not only on its microbiological activity in vitro, but also on the rate at which it is deacetylated in the doby and the activity of the resulting deacetyl compound.