Pyrrolidinedione derivatives as antibacterial agents with a novel mode of action

被引:90
作者
Pohlmann, J
Lampe, T
Shimada, M
Nell, PG
Pernerstorfer, J
Svenstrup, N
Brunner, NA
Schiffer, G
Freiberg, C [1 ]
机构
[1] Bayer AG, Dept Antiinfect Res, D-42096 Wuppertal, Germany
[2] Bayer AG, Dept Med Chem, D-42096 Wuppertal, Germany
关键词
pyrrolidine diones; moiramide B; andrimid; acetyl-CoA carboxylase; antibiotic;
D O I
10.1016/j.bmcl.2004.12.002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The pseudopeptide pyrrolidinedione natural products moiramide B and andrimid represent a new class of antibiotics that target bacterial fatty acid biosynthesis. Structure activity relationship (SAR) studies revealed a high degree of variability for the fatty acid side chain, allowing optimization of physicochemical parameters, and a restricted SAR for the pyrrolidinedione group, indicating major relevance of this subunit for efficient target binding. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1189 / 1192
页数:4
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