Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI)

被引：18
|
作者：
Sampson, Peter B. [1 ]
Picard, Christine [1 ]
Handerson, Sean [1 ]
McGrath, Teresa E. [1 ]
Domagala, Megan [1 ]
Leeson, Andrew [1 ]
Romanov, Vladimir [1 ]
Awrey, Donald E. [1 ]
Thambipillai, Dhushy [1 ]
Bardouniotis, Elias [1 ]
Kaplan, Nachum [1 ]
Berman, Judd M. [1 ]
Pauls, Henry W. [1 ]
机构：
[1] Affinium Pharmaceut Inc, Toronto, ON M8X 1Y9, Canada
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 18期
关键词：
Enoyl-ACP reductase; Naphthyridinone; FATTY-ACID BIOSYNTHESIS; TARGET;
D O I：
10.1016/j.bmcl.2009.07.129
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most potent FabI inhibitors yet described. The structural model of 14a bound to E. coli FabI is shown. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5355 / 5358
页数：4
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