Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships.

Lee SK; Choi KH; Lee SJ; Suh SW; Kim BM; Lee BJ

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Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships.

机译：具有逆酰胺骨架的肽去甲酰基酶抑制剂：合成与构效关系。

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Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies. Reported herein are the synthesis and structure-activity relationship studies of retro-amide inhibitors based on actinonin, a naturally occurring PDF inhibitor. Analysis of the structure-activity relationships led to the discovery of 7a, which exhibits potent enzyme inhibition and antibacterial activity against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.

机译：肽去甲酰基化酶（PDF）是一种金属蛋白酶，可催化从新合成的蛋白质中去除甲酰基。因此，抑制PDF活性被认为是最有效的抗生素策略之一。本文报道的是基于肌动蛋白（一种天然存在的PDF抑制剂）的逆酰胺抑制剂的合成和构效关系研究。对结构活性关系的分析导致了7a的发现，它对肺炎链球菌，流感嗜血杆菌和卡他莫拉菌表现出有效的酶抑制作用和抗菌活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第15期|共3页
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Lee SK; Choi KH; Lee SJ; Suh SW; Kim BM; Lee BJ;
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1. Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships. [J] . Lee SK, Choi KH, Lee SJ, Bioorganic and Medicinal Chemistry Letters . 2010,第15期

机译：具有逆酰胺骨架的肽去甲酰基酶抑制剂：合成与构效关系。
2. Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships. [J] . Lee SK, Choi KH, Lee SJ, Bioorganic and Medicinal Chemistry Letters . 2010,第15期

机译：具有逆酰胺骨架的肽去甲酰基酶抑制剂：合成与构效关系。
3. Peptide deformylase inhibitors with non-peptide scaffold: synthesis and structure-activity relationships. [J] . Lee SK, Choi KH, Lee SJ, Bioorganic and Medicinal Chemistry Letters . 2011,第1期

机译：具有非肽支架的肽去甲酰基酶抑制剂：合成与构效关系。
4. In-vivo assay of peptide deformylase inhibition based on MALDI-MS of whole bacterial cells [C] . Rachel R. Ogorzalek Loo, Ruth VanBogelen, Erin Schiller, Meeting of the American Electrophoresis Society . 2002

机译：基于全细菌细胞MALDI-MS的肽脱色酶抑制的体内测定
5. Part I. Isolation of natural product inhibitors and synthesis of inhibitors of signal transduction. Part II. Structure-activity relationship for a series of glycosidase inhibitors. [D] . Fraser, Rebecca Dawn. 1993

机译：第一部分：天然产物抑制剂的分离和信号转导抑制剂的合成。第二部分一系列糖苷酶抑制剂的构效关系。
6. N-Heterocyclic analogues as peptide deformylase inhibitors: Molecular modeling synthesis and antibacterial evaluation [O] . Anuradha Singh, Madhu Yadav, Preeti Singh, 2014

机译：N-杂环类似物作为肽去甲酰基酶抑制剂：分子模拟合成和抗菌评估
7. Macrocyclic Inhibitors for Peptide Deformylase: A Structure-Activity Relationship Study of the Ring Size [O] . -1

机译：肽脱晶体的大环抑制剂：环尺寸的结构 - 活性关系研究

Peptide deformylase inhibitors with retro-amide scaffold: synthesis and structure-activity relationships.

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