CAJ | 학술논문

为寻找能抵抗耐药酶作用的氨基糖苷类抗生素,本文对卡那霉素A的3'-OH,4'-OH和2"-OH位点进行了修饰.合成路线中的关键中间体为引入双苄叉保护基的卡那霉素A衍生物.目标羟基通过苄基化,甲基化和烯丙基化的方法进行修饰.最后通过多步反应脱保护,得到目标产物.活性结果显示,目标产物对敏感菌和耐药菌未显示出良好的抗菌活性.
위심조능저항내약매작용적안기당감류항생소,본문대잡나매소A적3'-OH,4'-OH화2"-OH위점진행료수식.합성로선중적관건중간체위인입쌍변차보호기적잡나매소A연생물.목표간기통과변기화,갑기화화희병기화적방법진행수식.최후통과다보반응탈보호,득도목표산물.활성결과현시,목표산물대민감균화내약균미현시출량호적항균활성.
The 3'-OH, 4'-OH and 2"-OH of kanamycin A were modified in search of new aminoglycosides to overcome resistant enzymes, ANTs and APHs. The key intermediate was a dibenzylidene-protected derivative of kanamycin A. The aimed sites were masked by benzyl, methyl and allyl groups. Multi-step reactions gave the desired aminoglycoside derivatives but showed less antibiotic activity than kanamycin A.