699012-73-2Relevant academic research and scientific papers
Potent and selective inhibitors of bacterial methionyl tRNA synthetase derived from an oxazolone-dipeptide scaffold
Tandon, Manish,Coffen, David L.,Gallant, Paul,Keith, Dennis,Ashwell, Mark A.
, p. 1909 - 1911 (2004)
The preparation and structure-activity relationships (SARs) of potent and selective small molecule inhibitors of bacterial methionyl-tRNA synthetase (MetRS) derived from an oxazolone-dipeptide scaffold are described. Examples combine Staphylococcus aureus MetRS (SaMetRS) potency with selectivity over human MetRS. As a result of the SAR expansion compound 14a was identified, as a potent SaMetRS inhibitor (IC50=18 nM) having moderate inhibition of MetRS derived from Enterococci faecalis (IC50=3.51 μM).
