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Parallel solid synthesis of inhibitors of the essential cell division FtsZ enzyme as a new potential class of antibacterials

Authors
Publisher
Elsevier Ltd
Publication Date
Volume
15
Issue
3
Identifiers
DOI: 10.1016/j.bmc.2006.11.015
Keywords
  • Parallel Synthesis
  • Gtp Analogues
  • Pseudomonas Aeruginosaftsz Inhibitors
  • Staphylococcus Aureus
Disciplines
  • Biology
  • Design

Abstract

Abstract As a model system for designing new inhibitors of bacterial cell division, we studied the essential and highly conserved FtsZ GTPase from Pseudomonas aeruginosa. A collection of GTP analogues were prepared using the solid-phase parallel synthesis approach. The synthesized GTP analogues inhibited the GTPase activity of FtsZ with IC 50 values between 450 μM and 2.6 mM, and 5 compounds inhibited Staphylococcus aureus growth in a biological assay. The FtsZ spectrophotometric assay developed for screening of synthesized compounds is the first step in identification of antibacterials targeting the bacterial cell division essential proteins.

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