Application of the Suzuki-Miyaura cross-coupling to increase antimicrobial potency generates promising novel antibacterials

被引:37
作者
Haug, Bengt Erik
Stensen, Wenche
Svendsen, John S.
机构
[1] Univ Tromso, Dept Chem, N-9037 Tromso, Norway
[2] Lytix Biopharma AS, N-9294 Tromso, Norway
关键词
cationic antimicrobial peptide; Suzuki-Miyaura coupling; antibacterial drugs;
D O I
10.1016/j.bmcl.2006.12.049
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Antimicrobial peptides have been recognized as a novel class of antibiotics, and several candidates are currently in clinical trials. In this work, a tripeptide derivative containing 4-iodo phenylalanine has been derivatized through the Suzuki-Miyaura cross-coupling. This has enabled the rapid and efficient synthesis of an array of tripeptide derivatives encompassing novel biaryl moieties. The peptide derivatives show high activity against Gram-positive bacteria. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2361 / 2364
页数:4
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