Macrolide antibiotics, process for their preparation, inter alia by fermentation, and pharmaceutical compositions containing them
申请人:SCHERING CORPORATION
公开号:EP0033433A1
公开(公告)日:1981-08-12
Disclosed are novel macrolide antibiotics of the general formula
wherein R is H or OH; M is 0 or (H,OH); Z is the group of formula II,
-CH7OH or groups which may be derived therefrom; A represents a double bond between carbon atoms of positions 12 and 13 or, together with the carbon atoms of positions 12 and 13, an oxirane ring. B represents a double bond between the carbon atoms of positions 10 and 11 or together with the carbon atoms of positions 10 and 11 the group -CH2-CH(O')-or-CH2-CH(O2)- and the non-toxic pharmaceutically acceptable ester and acid addition salts thereof.
The novel antibiotic complex designated antibiotic AR-5 of the formula
(falling within the scope of formula I), wherein R is hydrogen or hydroxy, and A represents a double bond or together with the carbon atoms of positions 12 and 13 an oxirane ring, can be produced by fermentation of a new species of the genus Micromonospora. which is Micromonospora Polytrota (e.g. NRRL 12066) The other compounds of formula I can be derived from the compounds of antibiotic AR-5 complex
The compounds shown antibacterial activity. The gentamycine C complex is also produced by mic- romonospora polytrota NRRL 12066
公开了通式如下的新型大环内酯类抗生素
其中 R 是 H 或 OH;M 是 0 或 (H,OH);Z 是式 II 的基团、
-A 代表位置 12 和 13 的碳原子之间的双键,或与位置 12 和 13 的碳原子一起构成环氧乙烷环。B 代表位置 10 和 11 的碳原子之间的双键,或与位置 10 和 11 的碳原子一起代表基团-CH2-CH(O')-或-CH2-CH(O2)-及其无毒的药学上可接受的酯和酸加成盐。
新型抗生素复合物命名为抗生素 AR-5,其式为
(属于式 I 的范围),其中 R 是氢或羟基,A 代表双键或与第 12 位和第 13 位的碳原子一起代表环氧乙烷环,可通过小孢子菌属的一个新物种发酵制得,该新物种是 Polytrota 小孢子菌(例如 NRRL 12066)。
显示出抗菌活性的化合物。NRRL 12066 也能产生庆大霉素 C 复合物。