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点击化学法构建雷帕霉素衍生物。第 3 部分：具有腺嘌呤苯侧链的衍生物的扩展足迹分析和对耐甲氧西林金黄色葡萄球菌（MRSA）的优异抑制作用。

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.

机构信息

Nucleic Acid Center, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, 5230 Odense M, Denmark.

Nucleic Acid Center, Department of Biochemistry and Molecular Biology, University of Southern Denmark, 5230 Odense M, Denmark.

出版信息

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1043-6. doi: 10.1016/j.bmcl.2014.01.019. Epub 2014 Jan 15.

DOI:10.1016/j.bmcl.2014.01.019
PMID:24486133
Abstract

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.

摘要

从我们之前的研究中筛选了 5 种有前途的截短侧耳素衍生物，它们都在不同的连接子上含有腺嘌呤，并补充了 2 种新的化合物。通过广泛的化学足迹分析证实了与大肠杆菌核糖体的结合。在两种金黄色葡萄球菌菌株上研究了抑制细菌生长的能力，并与截短侧耳素药物泰妙菌素和沃尼妙林进行了比较。其中 3 种化合物的效果类似于泰妙菌素，1 种化合物的效果类似于沃尼妙林。

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