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doi:10.1016/j.bmcl.2005.03.003 
Copyright © 2005 Elsevier Ltd All rights reserved.
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Richard L. Jarvesta, 
, 
, Symon G. Erskineb, Andrew K. Forresta, Andrew P. Fosberrya, Martin J. Hibbsa, Joanna J. Jonesa, Peter J. O’Hanlona, Robert J. Shepparda and Angela Worbya
Received 13 December 2004;
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Abstract
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.
Graphical abstract
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified an ethanolamine 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.
