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Synthesis and antibacterial activity of C12 des-methyl ketolides
Authors:Lin Xiaodong  Rico Alice C  Chu Daniel T  Carroll Georgia L  Barker Lynn  Shawar Ribhi  Desai Manoj C  Plattner Jacob J
Institution:Small Molecule Drug Discovery, Biopharma Research, Chiron Corporation, Emeryville, CA 94608, USA. xiaodong_lin@chiron.com
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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