Synthesis and biological properties of macrolactam analogs of the natural product macrolide (-)-A26771B

被引:17
|
作者
Canova, Sophie [2 ]
Lepine, Renaud [1 ]
Thys, Amber [3 ]
Baron, Anne [2 ]
Roche, Didier [2 ]
机构
[1] Galapagos, F-93230 Romainville, France
[2] Edelris, F-69003 Lyon, France
[3] Galapagos, Ind Pk Mechelen Noord, B-2800 Mechelen, Belgium
关键词
Natural products; (-)-A26771B; Antibacterial; Macrolactams; Metathesis; ANTIBIOTIC (-)-A26771B; CROSS METATHESIS; A26771B; RUCL2(=CHR)(PR(3))(2);
D O I
10.1016/j.bmcl.2011.06.073
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Promising synthetic derivatives of macrolactone natural product (-)-A26771B have been designed and synthesized both from semisynthesis and total synthesis. Further optimization led to the first synthesis of macrolactam analogs of (-)-A26771B with improved antibacterial activity and metabolic stability. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4768 / 4772
页数:5
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