The first potent inhibitors of glutamate racemase (MurI) enzyme that show whole cell antibacterial activity are described. Optically pure 4-substituted d-glutamic acid analogues with (2 R, 4 S) stereochemistry and bearing aryl-, heteroaryl-, cinnamyl-, or biaryl-methyl substituents represent a novel class of glutamate racemase inhibitors. Exploration of the d- Glu core led to the identification of lead compounds (-)-8 and 10. 2-Naphthylmethyl ...