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7 beta-[2-(2-Aminothiazol-4-yl)acetamido]-7 alpha-methoxycephalosporins were synthesized both by acylation of the 7 beta-amino-7 alpha-methoxycephalosporin compound (VIII) and a new direct acyl-exchange reaction of 7 alpha-methoxy-7 beta-phosphoramido compound (VII). Some of these compounds (IXa, IXb) showed higher antibacterial activity than the 7 alpha-unsubstituted compound against beta-lactamase-producing strains of Serratia marcescens and Proteus vulgaris.

journal of antibiotics

Synthesis and structure-activity relationships of 7.BETA.-[2-(2-aminothiazol-4-yl)acetamido]-cephalosporin derivatives. II. Synthesis and antibacterial activity of 7.BETA.-[2-(2-aminothiazol-4-yl)acetamido]-7.ALPHA.-methoxycephalosporins.