Teaching code

4S011740

Teacher

Giovanni Marzaro

Coordinator

Giovanni Marzaro

Credits

9

Language

Italian

Scientific Disciplinary Sector (SSD)

CHIM/08 - PHARMACEUTICAL CHEMISTRY

Period

PRIMO SEMESTRE dal Oct 6, 2025 al Dec 20, 2025.

Courses Single

Not Authorized

Lessons timetable Moodle Seminars 0

Learning objectives

At the end of the course the student:
• will have acquired notions which allow him to understand the molecular mechanism of action of a drug and in particular the types of bonds and the steric factors involved in the drug-molecular target interaction;
• will know the main classes of drugs that interact with targets located in host cells and drugs that interact with neurotransmitter receptors;
• will be able to apply the knowledge learned to understand their general synthesis, chemical-physical properties, mechanisms of action, structure-activity relationships

Prerequisites and basic notions

In order to fully understand the topics that will be covered in the course of "medicinal chemistry I" it is essential that students have already acquired knowledge of:
- general and inorganic chemistry, with particular reference to the concepts of: acidity/basicity (acidity constants, Ka and pKa, calculation of the pH of solutions containing weak acids or weak bases, concept of buffer solution and calculation of the pH of a buffer solution given the concentrations of the acid and basic species in solution and their pKa value); complexation of ions; oxidation-reduction reactions; interactions between ions.
- organic chemistry, with particular reference to the concepts of: functional groups and their electronic properties; acid/base properties of the main functional groups; reactivity and stability of esters and amides; concept of lipophilicity and hydrophilicity; types of intermolecular bond (polar, apolar interactions, hydrogen bridges, formation of dipoles, Van der Waals interactions); main reactions of functional groups; concept of electron-withdrawing and electron-donating effect; nomenclature of organic molecules; chemistry of the main heterocyclic compounds; chemistry of sugars and lipids.
- biochemistry and biology, with particular reference to the concepts of: biological macromolecule, function and structure of proteins and nucleic acids; enzyme and enzymatic catalysis; co-factor; allostery; cellular compartments; distinction between prokaryotes, eukaryotes, fungi, viruses and their respective characteristics.
- microbiology, with particular reference to the main characteristics of bacterial cells and virions; mechanisms of infection of the organism.
In the course of medicinal chemistry I, all the concepts considered as prerequisites will be widely used to describe the mechanism of action of drugs and to define the basis for their correct use in clinical practice. These concepts, therefore, will find a practical connotation in the drug sciences

Program

General information on medicinal chemistry: stages of drug development; general concept of drug and principle of operation; concept of agonist, antagonist, allosteric modulator, inhibitor; affinity, efficacy, selectivity; phases of drug action; chemical properties that determine the action of the drug; acidity and basicity, solubility in water, drug partition coefficient; types of drug-target bond; chemical properties and relationship with the route of administration; drug targets; metabolic reactions; bioisosterics; prodrugs.
Disinfectants and antiseptics: classes and mechanism of action
Antibacterial drugs: classes, mechanism of action, resistance phenomena, future prospects
Antifungal drugs: classes, mechanism of action
Antiparasitic drugs: classes, mechanism of action; antimalarial, antiprotozoal, anthelmintic, antiectoparasitic drugs
Antiviral drugs: classes, mechanism of action; classification according to the type of virus
Antitumor drugs: classes, mechanism of action; Classical chemotherapeutic drugs, drugs for targeted therapy
General and local anesthetic drugs: classification and mechanism of action

Bibliography

Didactic methods

The teacher will use: a) lectures; b) classroom exercises on fictional molecules, from which to derive the main chemical properties of interest in terms of use/administration; c) classroom exercises on fictional molecules that can ideally have activities belonging to the classes of drugs covered by the program; d) classroom exercises on hypothetical cases of interactions between drugs and foods of practical interest

Learning assessment procedures

Written exam (mandatory) lasting three hours with:
- 14 multiple choice questions on the entire program. A total of 0 to 14 points will be assigned (for each question: 0 for no answer; +1 for correct answer; -0.25 for incorrect answer).
- 4 open questions (one question on antibacterials; one question on antifungals or antiparasitics; one question on antivirals; one question on antitumor drugs). One of the 4 questions may also include the calculation of chemical parameters of a drug (for example: logP, solubility in water, degree of protonation in a particular district of the body). In this case, the reference tables shown in class will be made available, as well as any simplified general calculation formulas. A total of 0 to 16 points will be assigned (for each question: from 0 to 4 points).

Oral exam (optional, but strongly recommended for written scores lower than 20/30), consisting of:
- 1-2 questions that may concern any topic covered in the course. Up to a maximum of 2 additional points will be awarded.

A written score lower than 18/30 does not entitle the student to the oral exam and will therefore result in failure to pass the exam.

There will be no ongoing assessments.

Further details on the exam procedures, as well as examples of questions (both written and oral) will be provided by the teacher at the beginning, halfway through and at the end of the course.

Evaluation criteria

In multiple choice questions (written exam): correctness of the answer. Maximum score: 14/30

In open questions (written exam): correctness of the answer, quality of the presentation, use of correct scientific terminology, correct application of calculation formulas (if applicable). Maximum score: 16/30

In the optional oral exam questions: correctness of the answer, ability to create any connections between different but related topics, use of correct scientific terminology, quality of the presentation. Maximum score: 2/30

Criteria for the composition of the final grade

The overall grade of the exam will be given by the sum of the scores obtained in the written exam (max: 30/30) and in the oral exam (max: +2). Honors (30/30L) will be awarded upon reaching 32/30 points. To achieve honors, it is therefore necessary to obtain 30 points in the written exam and take the oral exam obtaining 2 points. For details on the attribution of scores for the written and oral exams, see the section "learning assessment methods"

Exam language

Italiano