3-Keto-9-O-substituted oxime derivatives of 6-O-methyl erythromycin A synthesis and in vitro activity.
A series of 3-keto-9-O-substituted oxime derivatives of 6-O-methyl erythromycin A were prepared with a novel synthetic route, which include 6 reaction steps--oximation, protection, hydrolysis, oxidation, deprotection and addition. The antibacterial activity of these compounds were tested in vitro against both erythromycin-susceptible and erythromycin-resistant organisms. Several of these derivatives showed improved antibacterial activity against some erythromycin-resistant organisms as compared to erythromycin A.
Shengxi
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C
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing. chenshengxi@sina.com
Xiandong
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X
Lanxiang
Y
Y
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004917:Erythromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests
C040934:6-O-methylerythromycin A; D000900:Anti-Bacterial Agents; D004917:Erythromycin