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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]

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