申请人:KYOWA HAKKO KOGYO CO., LTD.
公开号:EP0076463A2
公开(公告)日:1983-04-13
β-Lactam compounds represented by the general formula:
(wherein X represents CH2, S or 0; Y represents a hydroxyl group, a lower alkanoyloxy group or a lower alkoxycarbonyloxy group; W is a group represented by CH2, NH,
A is a phenyl group, a naphthyl group, or a monocyclic or dicyclic heterocyclic group, respectively substituted by (Y)n; R4 and R5 each are a hydrogen atom, a lower alkyl group, or a cycloalkylidene group with a carbon atom combined therewith; ℓ is 0 or an integer of 1, 2 or 3; m is 0 or 1; n is 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 0;Y 代表羟基、低级烷酰氧基或低级烷氧基羰酰氧基;W 是由 CH2、NH、
A 是分别被 (Y)n 取代的苯基、萘基或单环或双环杂环基团;R4 和 R5 分别是氢原子、低级烷基或带有一个碳原子的亚环烷基;ℓ 是 0 或 1、2 或 3 的整数;m 是 0 或 1;n 是 1、2、3、4 或 5 的整数;以及 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,尤其是包括铜绿假单胞菌、脓疱疮假单胞菌和各种肠杆菌在内的革兰氏阴性细菌具有很强的抗菌活性。