Synthesis and structure-activity relationships of 7.Beta.-[2- (2-aminothiazol-4-yl) acetamido]-cephalosporin derivatives. I. Synthesis and antibacterial activity of 7.Beta.-[2-alkyl-and 2-hydroxy-2- (2-aminothiazol-4-yl) -acetamido]cephalosporins

Ochiai, M.; Morimoto, A.; Matsushita, Y.; Kaneko, T.; Kida, M.

The Journal of Antibiotics 33(9): 1005-1013


DOI: 10.7164/antibiotics.33.1005
Accession: 068515839

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2-Alkyl- and 2-hydroxy derivatives of 7 beta-[2-aminothiazol-4-yl)acetamido]cephalosporins were synthesized to improve the antibacterial activity of the parent compounds especially against beta-lactamase-producing organisms. Some of these compounds showed an increase in activity against Serratia marcescens (Xb, XXIIIa) and Enterobacter cloacae (Xb, XIV). The 2,2-dimethyl derivative (XXVIIIb) showed a definite loss of activity.