Document Report Card

Basic Information

ID: ALA1147517

Journal: Bioorg Med Chem Lett

Title: Potent and selective inhibitors of bacterial methionyl tRNA synthetase derived from an oxazolone-dipeptide scaffold.

Authors: Tandon M, Coffen DL, Gallant P, Keith D, Ashwell MA.

Abstract: 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 (IC(50)=18 nM) having moderate inhibition of MetRS derived from Enterococci faecalis (IC(50)=3.51 microM).

CiteXplore: 15050625

DOI: 10.1016/j.bmcl.2004.01.094