C12去甲基酮内酯的合成及其抗菌活性
Synthesis and antibacterial activity of C12 des-methyl ketolides.
作者信息
Lin Xiaodong, Rico Alice C, Chu Daniel T, Carroll Georgia L, Barker Lynn, Shawar Ribhi, Desai Manoj C, Plattner Jacob J
机构信息
Small Molecule Drug Discovery, Biopharma Research, Chiron Corporation, Emeryville, CA 94608, USA.
出版信息
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4692-6. doi: 10.1016/j.bmcl.2006.05.104. Epub 2006 Jun 19.
PMID:16784845
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.
摘要
C(12) 去甲基酮内酯的合成方法得以发展，其特点是通过分子内环氧化合物的形成/消除过程来构建C(12) 立体中心。这些酮内酯对多种关键呼吸道病原体具有强效活性，包括耐红霉素的含erm和mef基因的肺炎链球菌菌株。
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