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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 16期

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

页码：4768 / 4772

页数：5

共 19 条

[1]

[Anonymous], 2010, DICT NATURAL PRODUCT

[2] BIOSYNTHESES OF ANTIBIOTIC A26771B BY PENICILLIUM-TURBATUM AND DEHYDROCURVULARIN BY ALTERNARIA-CINERARIAE - COMPARISON OF STEREOCHEMISTRY OF POLYKETIDE AND FATTY-ACID ENOYL THIOL ESTER REDUCTASES [J].