9-Oxime-3-ketolides: modification at the C-11,12-diol moiety and antibacterial activities against key respiratory pathogens.
In the search for new types of ketolide antibiotics active against key respiratory pathogens including erythromycin-resistant strains, we conducted an extensive study on the modification at the C-11,12-diol moiety of 9-oxime-3-ketolide derivatives. Among the derivatives prepared, compound 6 with carbonate at the C-11,12 position was found to have potent antibacterial activities against erythromycin-resistant Staphylococcus aureus as well as other erythromycin-susceptible strains.
Discovery Research Laboratories, Shionogi & Co. Ltd., 12-4, Sagisu 5-chome, Fukushima-ku, Osaka 553-0002, Japan. takashi.nomura@shionogi.co.jp
Takashi
T
Nomura
Tatsuro
T
Yasukata
Yukitoshi
Y
Narukawa
Kouichi
K
Uotani
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D004917:Erythromycin / Q000494:pharmacology; D048628:Ketolides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D010091:Oximes / Q000737:chemistry*; D012137:Respiratory System / Q000382:microbiology*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000472:pathogenicity
D000900:Anti-Bacterial Agents; D048628:Ketolides; D010091:Oximes; D004917:Erythromycin