OVERVIEW

Pharmaceutical and Toxicological Chemistry studies the design, synthesis, structures, structure-activity relationships (SAR), mechanisms of action, fields of application and secondary effects of drugs. In particular, Pharmaceutical and Toxicological Chemistry I is aimed at the study of disinfectant, antibacterial, antiprotozoal, antifungal and antitumor drugs.

AIMS AND CONTENT

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 common 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.

Any Student with documented Specific Learning Disorders (SLD), or with any special needs, shall reach out to the Lecturer(s) and to the dedicated SLD Representative in the Department ( Prof. Luca Raiteri, Luca.Raiteri@unige.it ) before class begins, in order to liaise and arrange the specific learning methods and ensure proper achievement of the learning aims and outcomes. VERY IMPORTANT: any request for compensatory tools and adaptations in the exam MUST be done within 10 working days before the date of the exam according to the instructions that can be found at https://unige.it/disabilita-dsa/comunicazioni.

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). Kinase inhibitors.

RECOMMENDED READING/BIBLIOGRAPHY

References:

1) Chimica Farmaceutica

Gasco, Gualtieri, Melchiorre, Editore CEA.

2) Principi di chimica farmaceutica,

William O. Foye Piccin-Nuova Libraria, 2021

3) Chimica Farmaceutica

PatricK, LG., Edises

4) Chimica farmaceutica

Costantino, Sbardella

TEACHERS AND EXAM BOARD

LESSONS

LESSONS START

https:// corsi.unige.it/corsi/11948/studenti-orario

Class schedule

The timetable for this course is available here: Portale EasyAcademy

EXAMS

EXAM DESCRIPTION

The exam consists of a written test (3 open questions) related to the first part of the syllabus (introductory part, antiseptics, antibiotics) and an oral interview concerning antitubercolars, antimalarials, antifungals, antivirals, antiparasitics, and antitumorals. The oral exam is conducted in the presence of two teachers, one of whom is the course instructor, and lasts between 30 and 60 minutes depending on the student's preparation. The final grade is the average of the two parts (written and oral).

ASSESSMENT METHODS

Will evaluate be evaluated: 1) the knowledge of the topics, 2) problems solving 3) the ability to use appropriate scientific language 4) the ability to connect the different topics covered in the course and also in the previous courses.

FURTHER INFORMATION

Please contact the teacher for additional information