Creating an antibacterial with in vivo efficacy: synthesis and characterization of potent inhibitors of the bacterial cell division protein FtsZ with improved pharmaceutical …

…, R Macdonald, NR Stokes, PK Chauhan…

Index: 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 Journal of Medicinal Chemistry, 2010 , vol. 53, # 10 p. 3927 - 3936

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Citation Number: 67

Abstract

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.