Medicinal Chemistry: The Molecular Basis of Drug Discovery

This medicinal chemistry course explores how chemists modify a molecule’s structure to design a safe and effective drug.

This course opens with a brief history of drug discovery and introduces the modern drug approval process.Then, we will transition to learning about receptors and enzymes, the body’s molecules most often targeted by drugs.We will also discuss the topics of pharmacokinetics (drug adsorption, elimination, and half-life) and metabolism. The course closes with units on how potential drug molecules are identified and subsequently optimized into safe and effective drugs.

Week 1: Pre-Regulatory Medicine and the Drug Approval Process Early natural products and synthetic molecules used as drugs Safety issues in the first drugs Modern drug discovery and approval process Intellectual property issues with drugs
Week 2: Drug Targets Structure of proteins Enzymes, enzymatic activity, and inhibition Receptors and molecules that modulate their activity Examination 1
Week 3: Pharmacokinetics Drug transport in the blood Clearance Volume of distribution Compartment modeling
Week 4: Metabolism Types of metabolic reactions Genetic and population effects Prodrugs Examination 2
Week 5: Binding, Structure, and Diversity Intermolecular forces Drug-target complementarity Molecular diversity and chemical libraries Combinatorial chemistry
Week 6: Lead Discovery Drug screening Filtering hits to find leads Existing drugs and natural products as leads
Week 7: Lead Optimization Functional group replacements Alkyl group replacements Isosteres and bioisosteres Peptidomimetics Examination 3