Discovery and development of new natural or synthetic organic compounds of biomedical utility is a critical component of medicinal chemical research. The Department of Medicinal Chemistry at the University of Kansas is among the pioneering departments to have focused on organic synthesis as a core area of its research activity. Since the days of its inception in the 1960s, the Department has been blessed with faculty members whose often-trailblazing ideas and research activities, both organic synthetic and medicinal chemical, have helped shape contemporary medicinal chemistry to its present state. More recently, research in the Department has expanded into the areas of biochemistry/peptide chemistry/chemical biology emphasizing the interactions of small molecules and peptides with larger biomolecules such as proteins and lipopolysaccharides. Working at the interface between chemistry and biology, researchers in the Department focus on the design, synthesis, and biological characterization of new and existing drugs as they interact with receptors and other cellular biochemical systems.