Cephalosporin antibiotics. II. Synthesis and biological properties of CS-461 and related compounds

  • J Antibiot (Tokyo). 1991 Aug;44(8):864-9. doi: 10.7164/antibiotics.44.864.
E Nakayama  1 ,  K Watanabe ,  M Miyauchi ,  K Fujimoto ,  S Muramatsu ,  H Yasuda ,  M Fukami ,  J Ide
Affiliations
  • 1. Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
PMID: 1917701 DOI: 10.7164/antibiotics.44.864
Abstract

The synthesis, structure-activity relationships, and biological properties of 3-thiazoliomethyl cephalosporins are described. 7-[2-(2-Aminothiazol-4-yl)-(Z)-2- methoxyiminoacetamido]-3-[5-(2-hydroxyethyl)-4-methylthiazoliomethyl+ ++]-3- cephem-4-carboxylate sulfate (CS-461) showed potent Antibacterial activity against a wide variety of bacteria both in vitro and in vivo. Furthermore, CS-461 exhibited significantly low acute toxicity in mice.

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