Synthetic Cephalosporins(第5報)3-Alkylthio-7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]cephalosporins及びその関連化合物の合成と抗菌活性

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3-Alkylthio-7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino) acetamido] cephalosporins (6 and 7) and the 3-methoxy analogues (10) were prepared by coupling diphenylmethyl 7-amino-3-alkylthio-3-cephem-4-carboxylate (1 and 2) or diphenylmethyl 7-amino-3-methoxy-3-cephem-4-carboxylate with (Z)-2-(2-tritylaminothiazol-4-yl)-2-(O-substituted oxyimino) acetic acid (4), followed by deprotection and subjected to examination of antibacterial activities. The pivaloyloxymethyl esters (8 and 9) of the compounds (6 and 7) were also prepared and oral activities of these esters were compared with those of the parent compounds (6 and 7). The cephalosporins (6a-j and 7a-c) had potent and wide antibacterial spectra against Gram positive and Gram negative bacteria which were comparable to those of cefixime or cefteram. Among them, the cephalosporins (6f and 7c) and the pivaloyloxymethyl esters (8b and 9b) had good in vivo efficacy in mice against infections of Escherichia coli No. 29 and especially 8b showed high urinary recovery in mice.
公益社団法人日本薬学会の論文
1989-12-25