596111-53-4Relevant academic research and scientific papers
Structure-based design of a macrocyclic inhibitor for peptide deformylase
Hu, Xubo,Nguyen, Kiet T.,Verlinde, Christophe L. M. J.,Hol, Wim G. J.,Pei, Dehua
, p. 3771 - 3774 (2007/10/03)
A macrocyclic, peptidomimetic inhibitor of peptide deformylase was designed by covalently cross-linking the P1′ and P3′ side chains. The macrocycle, which contains an N-formylhydroxylamine side chain as the metal-chelating group, was synthesized from a diene precursor via olefin metathesis using Grubbs's catalyst. The cyclic inhibitor showed potent inhibitory activity toward Escherichia coli deformylase (Ki = 0.67 nM) and antibacterial activity against both Gram-positive and Gram-negative bacteria (MIC = 0.7-12 μg/mL).
