Synthesis and antibacterial activity of C12 des-methyl ketolides |
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Authors: | Lin Xiaodong Rico Alice C Chu Daniel T Carroll Georgia L Barker Lynn Shawar Ribhi Desai Manoj C Plattner Jacob J |
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Affiliation: | Small Molecule Drug Discovery, Biopharma Research, Chiron Corporation, Emeryville, CA 94608, USA. xiaodong_lin@chiron.com |
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Abstract: | Synthesis of C(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C(12) stereocenter. These ketolides are potent against several key respiratory pathogens, including erythromycin resistant erm- and mef-containing strains of Streptococcus pneumoniae. |
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