LEARNING OUTCOMES

The course aims to study the design, synthesis and use of the drug. It then examines in depth the structural characteristics that affect the pharmacokinetics and mechanism of action of a wide range of compounds, as  topical and systemic antimicrobial, antiparasitic, antiviral and antitumor compounds. The aim of the course is to provide the student with the theoretical tools necessary to understand drug  design,  synthesis and use of the most commun pharmaceutical compounds used in therapy.

AIMS AND LEARNING OUTCOMES

The course aims to provide the student with the knowledge of drugs currently in use as disinfectants, antibacterials, antiprotozoal, antifungal and antitumor, their synthesis, mechanism of action and toxic effects. Syntheses, structure-activity relationships (SAR), optimization studies and action mechanisms of these therapeutic classes are reported. Furthermore, the course aims to provide students with the basic knowledge useful for design and synthesis of biologically active molecules.

Another fundamental objective of this course is the demonstration of the practical application in the field of pharmaceutical chemistry of all the knowledge acquired by the student during other courses, in particular those relating to general and organic chemistry and biochemistry.

At the end of the course the student will be able to recognize the main drugs of the categories listed in the program, describe their synthesis, structure-activity relationships, know the mechanisms of action and toxic effects.

PREREQUISITES

Knowledge of general inorganic chemistry, organic chemistry and biochemistry.

TEACHING METHODS

Theoretical frontal lessons during with slides available as teaching material on Aulaweb. These slides are a basis for detailed explanations by the teacher on the various topics of the course, in particular regarding syntheses and mechanism of action of discussed drugs. Both the frontal lessons and the exams can be carried out by team platform.

SYLLABUS/CONTENT

The program of the Pharmaceutical and Toxicological Chemistry I course is divided into various chapters, listed below.

General part - Definition of drug. Drug design. From design to the market. Pharmacokinetics. Proteins (enzymes, receptors, transport and structural proteins) as drug targets. Nucleic acids (DNA and RNA) as drug targets. Lipids and carbohydrates as drug targets.

Specific Classes of Drugs - Disinfectants and Antiseptics. Antibiotics and antibacterial chemotherapeutic agents: introduction, sulfonamides, nitro derivatives, fluoroquinolones, oxazolidinones, penicillins, cephalosporins, carbapemas, monobactams, beta lactamase inhibitors, peptide antibiotics, glycopeptides, phosphomycin, antibiotics. Anti-tuberculosis and anti-leprosy drugs. Antifungals. Antimalarials and other antiprotozoals. Anthelmintics. Antivirals against DNA viruses, antivirals against RNA viruses and anti-HIV. Anticancer drugs: classical chemotherapeutic agents, anticancer for hormone-dependent tumors. Anticancer with specific targets (enzyme inhibitors). Biotechn.  drugs. Vitamins.

RECOMMENDED READING/BIBLIOGRAPHY

Chimica Farmaceutica” Autori Gasco, Gualtieri, Melchiorre, Editore CEA