3-Arylpiperidines as potentiators of existing antibacterial agents

A Thorarensen, AL Presley-Bodnar, KR Marotti…

文献索引：Thorarensen, Atli; Presley-Bodnar, Alice L.; Marotti, Keith R.; Boyle, Timothy P.; Heckaman, Charlotte L.; Bohanon, Michael J.; Tomich, Paul K.; Zurenko, Gary E.; Sweeney, Michael T.; Yagi, Betty H. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 14 p. 1903 - 1906

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被引用次数: 40

摘要

Important resistance patterns in Gram-negative pathogens include active efflux of antibiotics out of the cell via a cellular pump and decreased membrane permeability. A 3-arylpiperidine derivative (1) has been identified by high-throughput assay as a potentiator with an IC50∼ 90μM. This report details the evaluation of the tether length, aryl substitution and the importance of the fluorine on antibiotic accumulation. Evaluation of various tether lengths ...