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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
来源:
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.
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页码:396 / 400
页数:5
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