An introduction to Medicinal Chemistry. The course aims to provide students with the general principles and the basic approaches of Medicinal Chemistry. In particular, the principal phases of drug action, the molecular mechanisms of drugs and the drug discovery and development process will be discussed.
Knowledge of the basic notions in medicinal chemistry, the most relevant issues of the drug action, the main techniques employed for the discovery and the development of an efficient drug, and the problems to deal with in this process. Knowledge of selected drug classes that have been discussed to explain the general concepts. Understanding medicinal chemistry activities in multidisciplinary frameworks and the progresses of a rapidly evolving discipline.
Principal phases of drug action (20 hours). Pharmaceutic, pharmacokinetic and pharmacodynamic phases. Pharmacokinetics: the processes of Absorption, Distribution, Metabolism, and Excretion of drugs. Pharmacodynamics: the molecular targets of drugs and the receptor concept. Structure and function of the receptors. Nature of drug-receptor interactions. Quantitative analysis of drug-receptor interactions and drug-induced biological responses (cell-free binding assays and cell-based functional assays). Definition of affinity, potency, efficacy, selectivity, therapeutic index. Definition of agonist, partial agonist, inverse agonist, antagonist. Receptor theory: models for drug-mediated receptor activation. Processes of signal transduction. Enzymes as drug targets.
Principal phases of drug discovery and development process (14 hours). Approaches for HIT and LEAD identification. Ligand efficiency metrics. LEAD modification and optimization: isostery and bioisostery, molecular simplification and complication, rigid analogs and prodrugs. Molecular modification of peptides. Recent advances in the design of peptidomimetics. Introduction to structure-activity relationship studies (QSAR) and computer-aided drug design methods (CADD). Computer lab lesson on the use of structural databases and virtual screening tools.
Analysis of selected pharmacological classes to illustrate the points discussed in the general section (14 hours).
Fundamental courses of organic chemistry of a Bachelor of Science in Chemistry or related fields.
- G. L. Patrick, An introduction to Medicinal Chemistry, Fifth or Sixth edition, Oxford University Press
- T. L. Lemke, D. A. Williams, V. F. Roche, S. W. Zito, Foye's Principles of Medicinal Chemistry, Seventh edition, Lippincott Williams & Wilkins, Wolters Kluwer
Knowledge of the organic chemistry at the level of a Bachelor of Science in Chemistry or related fields.
The exam will consist of a written test which aims to verify the preparation of the student on the course contents. The written examination will typically include 4-5 open questions: 1-2 questions will concern the phases of drug action, 1-2 questions will regard the drug discovery and development process, 1-2 questions will refer to drug classes discussed during the course. The evaluation of the student will be based on: the knowledge of the main issues concerning the phases of drug action and of drug discovery and development process, the ability to discuss in a critical and integrated way these general aspects in the specific examples given in the exam.
Language of instruction
Mode of teaching:
Traditional lessons will be integrated with additional teaching activities including computer lessons on the use of medchem databases and seminars on specific topics of the course.