Synthesis and biological activities of some 7-(1,2,4-oxadiazolylacetylamino) cephalosporins.

The synthesis and the physico-chemical properties of cephalosporin derivatives carrying an (1,2,4-oxadiazol-3-yl)- or (1,2,4-oxadiazol-5-yl)acetylamino moiety in position 7 are described. The effects of the presence of an amino or hydroxyl group on the oxadiazole ring are examined. Selected heterocyclicthiomethyl substituents are also introduced in the 3 position of the cephalosporin nucleus. In vitro antimicrobial activity and effectiveness in protecting against bacterial infection in the mouse are evaluated. Only compound (V b) was found to have slight activity when compared with cephalosporins in clinical use.