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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Lewis, Chad A.¹  Merkel, Janie²  Miller, Scott J.¹ 

[1] Yale Univ, Dept Chem, New Haven, CT 06520 USA

[2] Yale Univ, Ctr Chem Genom, New Haven, CT 06520 USA

关键词: Catalysis;    Natural product;    Erythromycin;    Peptide;    Antibiotic;   

DOI  :  10.1016/j.bmcl.2008.09.019

来源: Elsevier

【 摘 要 】

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. (C) 2008 Elsevier Ltd. All rights reserved.

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