Antimicrobial 7-(alpha-acylamino-alpha-arylacetamido)-3-(substituted methyl)cephalosporin compounds, their compositions and production
申请人:SUMITOMO CHEMICAL COMPANY, LIMITED
公开号:EP0035413A2
公开(公告)日:1981-09-09
Antimicrobial 7-(a-acylamino-a-arylacetamido)-3-(substituted methyl)cephalosporin compounds are represented by the formula (I)
wherein A is an optionally substituted pyridyl group, R1 and R2 are optional substituents and T is a 1-alkylene(carboxy, sulfo or dialkylamino), 1, 2, 3, 4-tetrazole-5-thio group or an optionally substituted N-pyridyl group. The COOH group may form a non-toxic salt.
Three condensation processes are provided for synthesis of compound (I) from preexisting cephalosporin compounds.
Pharmaceutical compositions contain the compound (I) and a carrier; parenteral administration is prefered. The compositions are effective against gram-positive and gram- negative bacteria.
抗菌 7-(a-酰氨基-a-芳基乙酰氨基)-3-(取代甲基)头孢菌素化合物由式 (I) 表示
其中 A 是任选取代的吡啶基,R1 和 R2 是任选取代基,T 是 1-亚烷基(羧基、磺基或二烷基氨基)、1,2,3,4-四唑-5-硫基或任选取代的 N-吡啶基。COOH 基团可形成无毒盐。
提供了三种缩合工艺,用于从已有的头孢菌素化合物中合成化合物 (I)。
药剂组合物包含化合物(I)和载体;首选肠外给药。组合物对革兰氏阳性菌和革兰氏阴性菌均有效。