Semisynthetic .Beta.-lactam antibiotics. I Synthesis and antibacterial activity of 7.Beta.- (2-aryl-2- (aminoacetamido) acetamido) cephalosporins

Furukawa, M.; Arimoto, M.; Nakamura, S.; Ejima, A.; Higashi, Y.; Tagawa, H.

The Journal of Antibiotics 39(9): 1225-1235


DOI: 10.7164/antibiotics.39.1225
Accession: 068516205

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The synthesis and in vitro structure-activity relationships of cephalosporins having dipeptides substituted with various aryl groups as the side chain at the C-7 position have been outlined. Of these compounds, 2-aminothiazol derivatives showed a broad spectrum of enhanced antibacterial activity, and 7 beta-[DL-2-(D-aminopropionamido)-2-(2-aminothiazol-4-yl)acet amido]-3- [(1-methyl-1H-tetrazol-5-yl)thiomethyl]ceph-3-em-4-carboxyli c acid was the most balanced of these active derivatives with respect to both Gram-positive and Gram-negative strains.