Synthetic Cephalosporins(第4報)7β-[(Z)-2-(2-Aminothiazol-4-yl)-2-(O-substituted oxyimino)acetamido]-3-(1,2,3-triazol-1-yl)methyl-3-cephem-4-carboxylic Acid及びその関連化合物の合成と抗菌活性

概要

論文の詳細を見る
Synthesis and oral activity of 7β-[(Z)-2-(2-aminothiazol-4-yl)-2-(O-substituted oxyimino)-acetamido]-3-(1,2,3-triazol-1-yl) methyl-3-cephem-4-carboxylic acid and its related compounds were described. 3-(1,2,3-Triazol-1-yl) methylcephalosporins have been prepared by the direct cycloaddition of acetylene to 3-azidomethylcephalosporins, which were obtained by nucleophilic substitution of 3-chloromethylcephalosporins with sodium azide in N, N-dimethylformamide. The cephalosporins (8a-c) had potent and wide antibacterial spectra against gram positive and gram negative bacteria which were comparable to those of cefixime or cefteram. Urinary recovery of 9a and 9b, pivaloyloxymethyl esters of 8a and 8b, were 9.2% and 3.5%, respectively, through oral administration in mice, exhibiting lower rate than that of cefteram pivoxyl (28%).
公益社団法人日本薬学会の論文
1989-12-25