New biological properties of tert-butyl cephalosporanate sulfones

Abstract tert -Butyl cephalosporanate 1,1-dioxides variously substituted in positions 7 and 3 were obtained from7-amino-deacetoxycephalosporanic acid (7-ADCA) and 7-aminocephalosporanic acid (7-ACA). It was found that the cephalosporins containing Aspirin and Diclofenac in a prodrug form in their 3-acyloxymethyl moiety release them after hydrolytic splitting of the β-lactam ring. They also demonstrated high efficacy as elastase inhibitors. Two of them stimulated the biosynthesis of nitric oxide in RAW 264.7 macrophages cells. The same effect observed in tumor and normal cells in the presence of cephalosporins was accompanied by cytotoxic effect in vitro.