期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 24, 页码 6231-6235出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.09.036
关键词
ketolide; macrolide; carbazate; macrolide-resistant bacteria
A novel series of ketolides containing heteroaryl groups that are linked to the erythronolide ring via a C6-carbazate functionality has been successfully synthesized. Careful modulation of the heteroaryl groups, the length and degree of saturation of the C6-carbazate linker, and the substituents present on each of the carbazate nitrogens led to compounds with potent activity against key bacterial respiratory pathogens. The best analogs of this series had in vitro and in vivo (sc dosing) profiles that were comparable to telithromycin. (c) 2006 Elsevier Ltd. All rights reserved.
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