Peptide deformylase inhibitors with activity against respiratory tract pathogens

Stephen P East; R Paul Beckett; Daniel C Brookings; John M Clements; Sheila Doel; Kenneth Keavey; Gilles Pain; Helen K Smith; Wayne Thomas; Alison J Thompson; Richard S Todd; Mark Whittaker

doi:10.1016/j.bmcl.2003.10.013

Peptide deformylase inhibitors with activity against respiratory tract pathogens

Bioorg Med Chem Lett. 2004 Jan 5;14(1):59-62. doi: 10.1016/j.bmcl.2003.10.013.

Authors

Stephen P East¹, R Paul Beckett, Daniel C Brookings, John M Clements, Sheila Doel, Kenneth Keavey, Gilles Pain, Helen K Smith, Wayne Thomas, Alison J Thompson, Richard S Todd, Mark Whittaker

Affiliation

¹ British Biotech Pharmaceuticals Limited, Watlington Road, Oxford OX4 6LY, UK. stephen.east@evotecoai.com

PMID: 14684298
DOI: 10.1016/j.bmcl.2003.10.013

Abstract

A series of analogues of the peptide deformylase (PDF) inhibitor BB-3497 where the P3' amide bond was replaced with a ketone functionality is described. The in vitro antibacterial profiling of these compounds revealed that they demonstrate activity against pathogens associated with respiratory tract infections.

MeSH terms

Amidohydrolases / antagonists & inhibitors*
Amidohydrolases / metabolism
Anti-Infective Agents / chemistry*
Anti-Infective Agents / pharmacology
Anti-Infective Agents / therapeutic use
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology
Enzyme Inhibitors / therapeutic use
Haemophilus influenzae / drug effects
Haemophilus influenzae / enzymology
Microbial Sensitivity Tests / statistics & numerical data
Moraxella catarrhalis / drug effects
Moraxella catarrhalis / enzymology
Respiratory Tract Infections / enzymology*
Respiratory Tract Infections / microbiology*
Streptococcus pneumoniae / drug effects
Streptococcus pneumoniae / enzymology

Substances

Anti-Infective Agents
Enzyme Inhibitors
Amidohydrolases
peptide deformylase