申请人:Shionogi & Co., Ltd.
公开号:US04203982A1
公开(公告)日:1980-05-20
Antibacterial 7.beta.-arylmalonamido-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acids of the formula: ##STR1## wherein Ar is a heterocyclic group or p-oxysubstituted phenyl; COB.sup.1 and COB.sup.2 are each a carboxy or protected carboxy group; and Het is an unsubstituted or substituted heterocyclic group. These compounds are prepared from, e.g., 7.beta.-amino-7.alpha.-methoxy-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acid derivatives by acylation with arylmalonic acid or reactive derivatives thereof. They are useful as an active ingredient in antibacterial pharmaceutical preparations.
抗菌7-β-芳基马隆酰胺基-7-α-甲氧基-3-杂环硫甲基-3-头孢-4-羧酸的化学式为:其中Ar是杂环基团或对氧基取代苯基;COB^1和COB^2分别是羧基或保护羧基;Het是未取代或取代的杂环基团。这些化合物可以通过与芳基马隆酸或其活性衍生物的酰化来制备,例如与7-β-氨基-7-α-甲氧基-3-杂环硫甲基-3-头孢-4-羧酸衍生物反应。它们可作为抗菌药物制剂中的活性成分。