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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.

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.

SUBMITTER: Haydon DJ

PROVIDER: S-EPMC2874265 | biostudies-literature | 2010 May

REPOSITORIES: biostudies-literature

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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.

Haydon David J DJ Bennett James M JM Brown David D Collins Ian I Galbraith Greta G Lancett Paul P Macdonald Rebecca R Stokes Neil R NR Chauhan Pramod K PK Sutariya Jignesh K JK Nayal Narendra N Srivastava Anil A Beanland Joy J Hall Robin R Henstock Vincent V Noula Caterina C Rockley Chris C Czaplewski Lloyd L

Journal of medicinal chemistry 20100501 10

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. ...[more]

PMID: 20426423

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