Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

Haydon, David J.; Bennett, James M.; Brown, David; Collins, Ian; Galbraith, Greta; Lancett, Paul; Macdonald, Rebecca; Stokes, Neil R.; Chauhan, Pramod K.; Sutariya, Jignesh K.; Nayal, Narendra; Srivastava, Anil; Beanland, Joy; Hall, Robin; Henstock, Vincent; Noula, Caterina; Rockley, Chris; Czaplewski, Lloyd

doi:10.1021/jm9016366.s001

jm9016366_si_001.pdf (325.44 kB)

Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

journal contribution

posted on 2015-12-16, 16:53 authored by David J. Haydon, James M. Bennett, David Brown, Ian Collins, Greta Galbraith, Paul Lancett, Rebecca Macdonald, Neil R. Stokes, Pramod K. Chauhan, Jignesh K. Sutariya, Narendra Nayal, Anil Srivastava, Joy Beanland, Robin Hall, Vincent Henstock, Caterina Noula, Chris Rockley, Lloyd Czaplewski

3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure−activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.

Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties

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