【文章名】Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ 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
作者
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
[摘要]: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.