A Novel Class of Inhibitors of Peptide Deformylase Discovered through High-Throughput Screening and Virtual Ligand Screening

Journal of Medicinal Chemistry
2004.0

Abstract

Peptide deformylase (PDF) has been identified as a promising antibacterial and herbicide target. A structurally novel class of inhibitors containing a 2-thioxo-thiazolidin-4-one heterocycle substituted by an arylidene group at the 5-position and a hexanoic acid side chain at the 3-position was discovered independently via high-throughput screening and virtual ligand screening. Data mining and analogue synthesis established a structure--activity relationship for the side chain region that is consistent with the docked structure.

Knowledge Graph

Similar Paper

A Novel Class of Inhibitors of Peptide Deformylase Discovered through High-Throughput Screening and Virtual Ligand Screening
Journal of Medicinal Chemistry 2004.0
Identification of novel potent bicyclic peptide deformylase inhibitors
Bioorganic & Medicinal Chemistry Letters 2004.0
Discovery and Refinement of a New Structural Class of Potent Peptide Deformylase Inhibitors
Journal of Medicinal Chemistry 2007.0
Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition
Bioorganic & Medicinal Chemistry Letters 2001.0
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment
Bioorganic & Medicinal Chemistry Letters 2016.0
Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria
European Journal of Medicinal Chemistry 2014.0
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections
Bioorganic & Medicinal Chemistry Letters 2019.0
Bacterial Peptide deformylase inhibition of cyano substituted biaryl analogs: Synthesis, in vitro biological evaluation, molecular docking study and in silico ADME prediction
Bioorganic & Medicinal Chemistry 2016.0
Synthesis and PDF inhibitory activities of novel benzothiazolylidenehydroxamic acid derivatives
Bioorganic & Medicinal Chemistry Letters 2003.0
Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase
Bioorganic & Medicinal Chemistry Letters 2011.0