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

[Image: see text] 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 inhibitor...

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Detalles Bibliográficos
Autores principales: 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
Formato: Texto
Lenguaje:English
Publicado: American Chemical Society 2010
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2874265/
https://www.ncbi.nlm.nih.gov/pubmed/20426423
http://dx.doi.org/10.1021/jm9016366
Descripción
Sumario:[Image: see text] 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.