β-ラクタム系抗生物質の薬学的研究(第12報)7β-[α-(4-Ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-substituted acetamido]-7α-methoxycephalosporanic Acid類の合成ならびに構造-活性相関

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New 7α-methoxycephalosporins, 7β-[α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-substituted acetamido]-7α-methoxycephalosporanic acids (Ia-p) were prepared. They showed a broad antibacterial spectrum, especially a strong antibacterial activity against gram-negative bacilli such as Pseudomonas aeruginosa and Serratia marcescens. In these compounds, 7β-[D (-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-phenylacetamido]-7α-methoxy-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylic acid (Ic), 7β-[D-(-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamido]-7α-methoxy-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylic acid (Id) and 7β-[D (-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(2-thienyl) acetamido]-7α-methoxy-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylic acid (Ig) were selected and evaluated for antibacterial activity, stability against β-lactamase, protective effects on experimental infections.
社団法人日本薬学会の論文
1982-07-25