Creating an Antibacterial with in Vivo Efficacy: Synthesis and Characterization of Potent Inhibitors of the Bacterial Cell Division Protein FtsZ with Improved Pharmaceutical Properties
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.
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关键词:
Animals Humans Mice Hepatocytes Staphylococcus aureus Caco-2 Cells Staphylococcal Infections Pyridines Thiazoles Bacterial Proteins
DOI:
10.1021/jm9016366
被引量:
年份:
2010
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