Novel chiral pyrrolidinone scaffolds derived from threonine with antibacterial activity

被引:21
作者
Anwar, Muhammad [1 ]
Cowley, Andrew R. [1 ]
Moloney, Mark G. [1 ]
机构
[1] Univ Oxford, Chem Res Lab, Dept Chem, Oxford OX1 3TA, England
关键词
DIVERSITY-ORIENTED SYNTHESIS; NATURAL-PRODUCTS; DRUG DISCOVERY; TETRAMIC ACIDS; SERINE; 16-METHYLOXAZOLOMYCIN; INHIBITORS; ALKYLATION; REACTIVITY; MOLECULES;
D O I
10.1016/j.tetasy.2010.04.064
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
The synthesis of chiral pyrrolidinones derived from threonine, making use of a Dieckmann or aldol ring closure, is described. Compounds were found to exhibit antibacterial activity, for which the correlation with various physiochemical parameters was examined. This chiral tetramate scaffold may provide a useful template for fragment-based drug design providing rapid access to novel antibacterial compound libraries. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1758 / 1770
页数:13
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