Title of article :
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Author/Authors :
Richard L. Jarvest، نويسنده , , Symon G. Erskine، نويسنده , , Andrew K. Forrest، نويسنده , , Andrew P. Fosberry، نويسنده , , Martin J. Hibbs، نويسنده , , Joanna J. Jones، نويسنده , , Peter J. O’Hanlon، نويسنده , , Robert J. Sheppard، نويسنده , , Angela Worby، نويسنده ,
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.
