852392-21-3Relevant articles and documents
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
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
, p. 2305 - 2309 (2007/10/03)
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.
