申请人:HOKURIKU SEIYAKU CO., LTD.
公开号:EP1323726A1
公开(公告)日:2003-07-02
Erythromycin derivatives or salt thereof having excellent antibacterial activity against atypical acid-fast mycobacteria and useful as antibacterial agent, which is represented by the following general formula:
wherein, R1 and R2 represent hydrogen atom, an alkyl group, a homocyclic or heterocyclic group, an alkyl group substituted with a homocyclic group, or an alkyl group substituted with a heterocyclic group or the like, or R1 and R2 may combine to form a homocycle or a heterocycle, R3 represents hydrogen atom or methyl group, R4 represents hydroxyl group or the like; R5 represents hydrogen atom, hydroxyl group or the like, R6 and R7 represent hydrogen atom, an alkyl group or the like; X represents NH or a group represented by N-O-R8, Y represents a group represented by O-C(=O)-R9, a cladinose derivative or the like, Z represents oxygen atom or sulfur atom, R8 and R9 represents an alkyl group, a homocyclic or heterocyclic group, an alkyl group substituted with a homocyclic group, or an alkyl group substituted with a heterocyclic group.
红霉素衍生物或其盐对非典型耐酸霉菌具有优异的抗菌活性,可用作抗菌剂,其通式如下:
其中,R1 和 R2 代表氢原子、烷基、同环基或杂环基、被同环基取代的烷基或被杂环基取代的烷基等,或 R1 和 R2 可结合形成同环或杂环,R3 代表氢原子或甲基,R4 代表羟基等;R5 代表氢原子、羟基或类似物,R6 和 R7 代表氢原子、烷基或类似物;X 代表 NH 或由 N-O-R8 表示的基团,Y 代表由 O-C(=O)-R9、克拉丁糖衍生物或类似物表示的基团,Z 代表氧原子或硫原子,R8 和 R9 代表烷基、同环基或杂环基、被同环基取代的烷基或被杂环基取代的烷基。