Document Report Card

ID: ALA1145063

Journal: J Med Chem

Title: Structure-based design of a macrocyclic inhibitor for peptide deformylase.

Authors: Hu X, Nguyen KT, Verlinde CL, Hol WG, Pei D.

Abstract: 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 (K(I) = 0.67 nM) and antibacterial activity against both Gram-positive and Gram-negative bacteria (MIC = 0.7-12 microg/mL).

CiteXplore: 12930137

DOI: 10.1021/jm034113f