A click chemistry approach to pleuromutilin derivatives. Part 3: Extended footprinting analysis and excellent MRSA inhibition for a derivative with an adenine phenyl side chain

被引：27

作者：

Dreier, Ida ^{[1
]}

Hansen, Lykke H. ^{[2
]}

Nielsen, Poul ^{[1
]}

Vester, Birte ^{[2
]}

机构：

[1] Univ Southern Denmark, Dept Phys Chem & Pharm, Nucle Acid Ctr, DK-5230 Odense M, Denmark

[2] Univ Southern Denmark, Dept Biochem & Mol Biol, Nucle Acid Ctr, DK-5230 Odense M, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 04期

基金：

美国国家科学基金会;

关键词：

Pleuromutilin derivatives; Antibiotics; Click chemistry; MRSA inhibition; Chemical footprinting; PEPTIDYL TRANSFERASE CENTER; TERMINAL ALKYNES; ANTIBIOTICS; TIAMULIN; RIBOSOME; BINDING; NUCLEOSIDES; AZIDES; RNA; FIT;

D O I：

10.1016/j.bmcl.2014.01.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Five promising pleuromutilin derivatives from our former studies, all containing adenine on various linkers, were supplemented with two new compounds. The binding to Escherichia coli ribosomes was verified by extensive chemical footprinting analysis. The ability to inhibit bacterial growth was investigated on two Staphylococcus aureus strains and compared to the pleuromutilin drugs tiamulin and valnemulin. Three of the compounds show an effect similar to tiamulin and one compound shows an excellent effect similar to valnemulin. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：1043 / 1046

页数：4

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