Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase

…, MJ Hibbs, JJ Jones, PJ O'Hanlon, RJ Sheppard…

文献索引：Jarvest, Richard L.; Erskine, Symon G.; Forrest, Andrew K.; Fosberry, Andrew P.; Hibbs, Martin J.; Jones, Joanna J.; O'Hanlon, Peter J.; Sheppard, Robert J.; Worby, Angela Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 9 p. 2305 - 2309

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被引用次数: 19

摘要

High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.