A drug discovery project has been successfully implemented in a first-year general, organic, and biochemistry (GOB) health science course and second-year organic undergraduate chemistry course. This project allows students to apply the fundamental principles of chemistry and biology to a problem of medical significance, practice basic laboratory skills, and understand the interdisciplinary aspect of the drug discovery platform. Students collectively synthesize a small library of antituberculosis compounds and subsequently screen them using a Kirby-Bauer disc diffusion assay for inhibitory activity against "Mycobacterium smegmatis", a known safe surrogate of "Mycobacterium" tuberculosis, the causative agent of tuberculosis. The last unit of the project involves students using PyMOL, a free computer program, to examine a cocrystal structure of the activated inhibitor-enzyme complex, allowing students to identify the molecular interactions responsible for the binding affinity.