Cephalosporin antibiotics. II. Synthesis and biological properties of CS-461 and related compounds |
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| Authors: | E Nakayama K Watanabe M Miyauchi K Fujimoto S Muramatsu H Yasuda M Fukami J Ide |
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| Affiliation: | Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. |
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| 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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