Synthesis and antibacterial activity of nocathiacin I analogues

被引:47
作者
Naidu, BN [1 ]
Sorenson, ME [1 ]
Matiskella, JD [1 ]
Li, WY [1 ]
Sausker, JB [1 ]
Zhang, YH [1 ]
Connolly, TP [1 ]
Lam, KS [1 ]
Bronson, JJ [1 ]
Pucci, MJ [1 ]
Yang, H [1 ]
Ueda, Y [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
关键词
nocathiacin I; antibacterial activity;
D O I
10.1016/j.bmcl.2006.03.079
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Stereoselective reduction of dehydroalanine double bond in nocathiacin 1 afforded the primary amide 2. Enzymatic hydrolysis of the amide 2 provided the carboxylic acid 3, which upon coupling with a variety of amines furnished amides 4-32. Some of these semi-synthetic derivatives have retained very good antibacterial activity and have improved aqueous solubility. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3545 / 3549
页数:5
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