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5''-修饰新霉素的合成及联合抗菌研究

Synthesis and combinational antibacterial study of 5''-modified neomycin.

作者信息

Zhang Jianjun, Keller Katherine, Takemoto Jon Y, Bensaci Mekki, Litke Anthony, Czyryca Przemyslaw Greg, Chang Cheng-Wei Tom

机构信息

Department of Chemistry and Biochemistry, Utah State University, Logan, UT 84322-0300, USA.

出版信息

J Antibiot (Tokyo). 2009 Oct;62(10):539-44. doi: 10.1038/ja.2009.66. Epub 2009 Jul 24.

DOI:10.1038/ja.2009.66
PMID:19629142
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2783947/
Abstract

A library of 5''-modified neomycin derivatives were synthesized for an antibacterial structure-activity optimization strategy. Two leads exhibited prominent activity against both methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Antibacterial activities were measured when combined with other clinically used antibiotics. Significant synergistic activities were observed, which may lead to the development of novel therapeutic practices in the battle against infectious bacteria.

摘要

为了优化抗菌结构与活性的策略，合成了一个5'-修饰的新霉素衍生物文库。两种先导化合物对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE）均表现出显著活性。当与其他临床使用的抗生素联合使用时，测定了其抗菌活性。观察到显著的协同活性，这可能会在对抗感染性细菌的斗争中促成新的治疗方法的开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/8465920523d4/nihms129306f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/bf9d395c84e9/nihms129306f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/9bac681d537c/nihms129306f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/4b0574647b3c/nihms129306f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/8465920523d4/nihms129306f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/bf9d395c84e9/nihms129306f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/9bac681d537c/nihms129306f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/4b0574647b3c/nihms129306f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dead/2783947/8465920523d4/nihms129306f4.jpg

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