This course provides an overview of topics central to the understanding and practice of contemporary medicinal chemistry. It illustrates the interplay of anatomy and physiology with the organic-, bio- and analytical chemistry of drugs in the body. Topics covered include physiological mechanisms and disease processes; cell structure and function; basic intermediary metabolism; basic principles underlying drug action including the physicochemical properties of drugs and how these affect the interaction of drugs with living systems; chemical and biological manipulation of the absorption, distribution, metabolism and excretion of drugs and prodrugs; kinetics and inhibition of enzymes and transporters; quantitation and molecular modeling of drug binding to targets. Prerequisite: One year of organic chemistry, one semester of biochemistry, and one college-level course in biology.