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大环肽基异羟肟酸酯作为肽脱甲酰基酶抑制剂的设计与合成

Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors.

作者信息

Shen Gang, Zhu Jinge, Simpson Anthony M, Pei Dehua

机构信息

Department of Chemistry, The Ohio State University, 100 West 18th Avenue, Columbus, OH 43210, USA.

出版信息

Bioorg Med Chem Lett. 2008 May 15;18(10):3060-3. doi: 10.1016/j.bmcl.2007.12.011. Epub 2007 Dec 10.

DOI:10.1016/j.bmcl.2007.12.011
PMID:18093832
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2430612/
Abstract

Macrocyclic peptidyl hydroxamates were designed, synthesized, and evaluated as peptide deformylase (PDF) inhibitors. The most potent compound exhibited tight, slow-binding inhibition of Escherichia coli PDF (K(I)(*)=4.4 nM) and had potent antibacterial activity against Gram-positive bacterium Bacillus subtilis (MIC=2-4 microg/mL).

摘要

设计、合成并评估了大环肽基异羟肟酸酯作为肽脱甲酰基酶（PDF）抑制剂。最有效的化合物对大肠杆菌PDF表现出紧密、慢结合抑制作用（K(I)(*) = 4.4 nM），并对革兰氏阳性菌枯草芽孢杆菌具有强效抗菌活性（MIC = 2 - 4 μg/mL）。

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本文引用的文献

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The evolution of peptide deformylase as a target: contribution of biochemistry, genetics and genomics.肽脱甲酰基酶作为一个靶点的演变：生物化学、遗传学和基因组学的贡献。
Biochem Pharmacol. 2006 Mar 30;71(7):1042-7. doi: 10.1016/j.bcp.2005.10.015. Epub 2005 Nov 11.
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Therapeutic potential of peptide deformylase inhibitors.肽脱甲酰基酶抑制剂的治疗潜力。
Expert Opin Investig Drugs. 2005 Sep;14(9):1107-16. doi: 10.1517/13543784.14.9.1107.
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Bacterial Peptide deformylase inhibitors: a new class of antibacterial agents.细菌肽脱甲酰基酶抑制剂：一类新型抗菌剂。
Curr Med Chem. 2005;12(14):1607-21. doi: 10.2174/0929867054367194.
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Macrocyclic inhibitors for peptide deformylase: a structure-activity relationship study of the ring size.肽脱甲酰基酶的大环抑制剂：环大小的构效关系研究
J Med Chem. 2004 Sep 23;47(20):4941-9. doi: 10.1021/jm049592c.
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Bioorg Med Chem Lett. 2003 Dec 1;13(23):4223-8. doi: 10.1016/j.bmcl.2003.07.020.
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