申请人:KYOWA HAKKO KOGYO CO., LTD
公开号:EP0075805A1
公开(公告)日:1983-04-06
β-Lactam compounds represented by the general formula:
(wherein X represents CH2, S or O; Y represents a hydroxyl group, lower alkanoyloxy group, amino group or substituted amino group; A represents a phenyl group, naphthyl group, or monocyclic or dicyclic heterocyclic group, respectively substituted by (Y)n; R4 and R5 each represent a hydrogen atom, lower alkyl group or cycloalkylidene group together with the carbon atom combined therewith; represents an integer of 0,1,2 or 3; m represents an integer of 0 or 1; and n represents an integer of 1, 2, 3, 4 or 5; and R1, R2 and R3 are groups often used in the conventional β-lactam compounds) have strong antimicrobial activities against a wide range of Gram positive and negative bacteria; particularly Gram negative bacteria including Pseudomonas aeruginosa, Pseudomonas sepatia and various Enterobacters.
由通式代表的β-内酰胺化合物:
(其中 X 代表 CH2、S 或 O;Y 代表羟基、低级烷酰氧基、氨基或取代氨基;A 代表苯基、萘基或分别被 (Y)n 取代的单环或双环杂环基团;R4 和 R5 分别代表氢原子、低级烷基或环亚烷基及其结合的碳原子;代表 0、1、2 或 3 的整数;m 代表 0 或 1 的整数;n 代表 1、2、3、4 或 5 的整数;R1、R2 和 R3 是常规 β-内酰胺化合物中常用的基团)对多种革兰氏阳性和阴性细菌具有很强的抗菌活性,尤其是革兰氏阴性细菌,包括铜绿假单胞菌、败血假单胞菌和各种肠杆菌。