Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, IN 46556, USA.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1302-5. doi: 10.1016/j.bmcl.2009.10.018. Epub 2009 Oct 8.
A series of novel oxazolidinone antibiotics having [2.2.1] and [2.2.2] bicyclic oxazine moieties at the C-5 side chain of the A-ring was synthesized by nitroso Diels-Alder reactions, from three linezolid analogs containing morpholine, piperazine and thiomorpholine, respectively, as the C-ring components. Subsequent N-O bond cleavage generated oxazolidinones with 4-amino cyclo-2-en-1-ol substituents. The in vitro antibacterial activities of these oxazolidinone analogs were evaluated.
通过硝基亚胺 Diels-Alder 反应，从三个分别含有吗啉、哌嗪和硫代吗啉作为 C 环组成部分的利奈唑胺类似物中合成了一系列具有[2.2.1]和[2.2.2]双环氧嗪环部分的新型恶唑烷酮抗生素，位于 A 环 C-5 侧链上。随后 N-O 键的断裂生成了具有 4-氨基环-2-烯-1-醇取代基的恶唑烷酮。评估了这些恶唑烷酮类似物的体外抗菌活性。
