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

C Paradis-Bleau, M Beaumont, F Sanschagrin…

Index: Paradis-Bleau, Catherine; Beaumont, Melanie; Sanschagrin, Francois; Voyer, Normand; Levesque, Roger C. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 3 p. 1330 - 1340

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Citation Number: 45

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 IC50 values between 450μM and 2.6 mM, and 5 compounds inhibited Staphylococcus aureus growth in a ...