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There is a well recognized need for new antibacterial agents to fight resistant bacteria,such as MRSA and VRE.The inhibition of novel essential cell-wall targets,such as glutamate racemase (MurI),provides a great opportunity to design the next generation of antibacterials.This talk will be focused on the recent efforts of discovering MurI inhibitors in Gram-positive bacteria and Gram-negative Helicobacter Pylori.The entire discovery process from High Throughput Screening (HTS),Lead Identification (LI) and Lead Optimization (LO) will be presented.Emphasis will be given to the demonstration of the power of HTS to discover allosteric enzyme inhibitors and Structural Activity Relationship (SAR) development employing Structure-Based Drug Design (SBDD)/Chemoinformatic tools during LI/LO Process.