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一系列红霉素类似物的催化位点选择性合成与评价

Catalytic site-selective synthesis and evaluation of a series of erythromycin analogs.

作者信息

Lewis Chad A, Merkel Janie, Miller Scott J

机构信息

Department of Chemistry, Yale University, 225 Prospect Street, New Haven, CT 06520-8107, USA.

出版信息

Bioorg Med Chem Lett. 2008 Nov 15;18(22):6007-11. doi: 10.1016/j.bmcl.2008.09.019. Epub 2008 Sep 9.

DOI:10.1016/j.bmcl.2008.09.019
PMID:18819795
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2669672/
Abstract

The generation of a series of analogs of erythromycin A (EryA, 2) is described. In this study, we compared two peptide-based catalysts-one originally identified from a catalyst screen (5) and its enantiomer (ent-5)-for the selective functionalization of EryA. The semi-synthetic analogs were subjected to MIC evaluation with two bacterial strains and compared to unfunctionalized EryA.

摘要

描述了一系列红霉素A(EryA,2)类似物的生成。在本研究中,我们比较了两种基于肽的催化剂——一种最初从催化剂筛选中鉴定出来(5)及其对映体(对映体-5)——用于EryA的选择性官能化。对这些半合成类似物用两种细菌菌株进行了最低抑菌浓度(MIC)评估,并与未官能化的EryA进行了比较。

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