NEW BIOLOGICAL PROPERTIES OF TERT-BUTYL CEPHALOSPORANATE SULFONES

tert-Butyl cephalosporanate I,l-dioxides variously substituted in posi tions 7 and 3 were obtained from 7-aminodeacetoxycephalosporanic acid (7-ADCA) and 7-aminocephalosporanic acid (7 ACA). It was found that th e cephalosporins containing Aspirin and Diclofenac in a prodrug form i n their 3-acyloxymethyl moiety release them after hydrolytic splitting of the beta-lactam ring. They also demonstrated high efficacy as elas tase inhibitors. Two of them stimulated the biosynthesis of nitric oxi de in RAW 264.7 macrophages cells. The same effect observed in tumor a nd normal cells in the presence of cephalosporins was accompanied by c ytotoxic effect in vitro. (C) Elsevier, Paris.