Skeletal Analogues of UCS1025A and B by Cyclization of Maleimides: Synthesis and Biological Activity

被引:2
|
作者
Ibbotson, Lewis T. [1 ]
Christensen, Kirsten E. [1 ]
Genov, Miroslav [2 ]
Pretsch, Alexander [2 ]
Pretsch, Dagmar [2 ]
Moloney, Mark G. [1 ,3 ]
机构
[1] Univ Oxford, Dept Chem, Chem Res Lab, 12 Mansfield Rd, Oxford OX1 3TA, England
[2] Oxford Antibiot Grp, Magdalen Ctr, Oxford Sci Pk, Oxford OX4 4GA, England
[3] Oxford Suzhou Ctr Adv Res, Bldg A,388 Ruo Shui Rd,Suzhou Ind Pk, Suzhou 215123, Jiangsu, Peoples R China
关键词
lactams; aldol reaction; ketene silyl ether; cyclization; antibiotics; ANTIBIOTICS; CJ-16,264; SCAFFOLDS; FAMILY; ACIDS;
D O I
10.1055/s-0040-1719876
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Application of a direct ring-closing approach which exploits an intramolecular aldol reaction with a ketene silyl acetal onto a remote imide function leading to the core skeleton of UCS1025A and B effectively provides access to small library of substituted analogues; of interest is their complete lack of antibacterial activity against MRSA (Gram+) and E. coli (Gram-) bacterial strains. © 2022 Georg Thieme Verlag. All rights reserved.
引用
收藏
页码:396 / 400
页数:5
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