Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article; Proceedings Paper

Shen, Gang¹  Zhu, Jinge¹  Simpson, Anthony M.¹  Pei, Dehua¹ 

[1] Ohio State Univ, Dept Chem, Columbus, OH 43210 USA

关键词: peptide deformylase;    antibacterial;    macrocycle;    inhibition;    hydroxamate;   

DOI  :  10.1016/j.bmcl.2007.12.011

来源: Elsevier

【 摘 要 】

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 mu g/mL). (c) 2007 Elsevier Ltd. All rights reserved.

【 授权许可】

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