Unit MEDICINAL CHEMISTRY I
- Course
- Industrial pharmacy
- Study-unit Code
- 65903809
- Curriculum
- In all curricula
- Teacher
- Oriana Tabarrini
- Teachers
-
- Oriana Tabarrini
- Hours
- 72 ore - Oriana Tabarrini
- CFU
- 9
- Course Regulation
- Coorte 2024
- Offered
- 2026/27
- Learning activities
- Caratterizzante
- Area
- Discipline farmaceutico-alimentari
- Sector
- CHIM/08
- Type of study-unit
- Obbligatorio (Required)
- Type of learning activities
- Attività formativa monodisciplinare
- Language of instruction
- Italian
- Contents
- Th preliminary part of the course will entail the study of how a drug is identified and designed, the chemical-physical properties and its structure-activity relationship. Then, the main classes of drugs will be described: anticholinergic, antiadrenergic, antihistaminic, CNS drugs (analgesics, antidepressants, sedative-hypnotics, anxiolytics, antipsychotics, anesthetics, anti-Parkinson) antiulcer. The structure, nomenclature, synthesis, therapeutic indications, main side effects, and metabolism are given for many of them.
- Reference texts
- Foye's Principi di Chimica Farmaceutica (Williams, Lemke) PICCIN Chimica Farmaceutica (Wilson & Gisvold) Chimica Farmaceutica (Casa Editrice Ambrosiana) Slides of lessons
- Educational objectives
- Medicinal chemistry I is the first of the three courses of medicinal chemistry provided by the degree in Chemistry and Technology of Drugs (CTF). While the course will give the students detailed knowledge on various classes of drugs with particular reference to those who act in the CNS, the main aim of the course will be in giving the students strong basis to understand every classes of therapeutic agents. The following knowledge will be acquired by the students:a)the relationship between structure and biological activity; b)the mechanism of action underlying the biological activity; c)the therapeutic option. In addition, the student will acquire the following abilities: a) suggest the best drug for a given pathology; b) synthesize some drugs among those studied; c) be able to go back to the structure knowing the chemical name. Moreover, the students will have an overview of how you can identify a drug, how to improve its chemical and physical properties, such as increasing the power and how to reduce side effects. In summary,this course aims to furnish the student a solid knowledge of the Medicinal Chemistry to be used as starting platform by the students who can use it to increase their knowledge and become able to analyze any classes of drugs independently.
- Prerequisites
- The medicinal chemistry is a complex course which entails the study of drugs. In particular, it studies how certain structures are able to impart biological activity. Being highly multidisciplinary, to attend the medicinal chemistry lessons, to understand the course contents as well as the aim of the course, previous knowledge of organic chemistry, biochemistry and pharmacology, are strongly required.
- Teaching methods
- Theoretical lessons in class with the help of slides. Some exercises on the synthesis of selected drugs and their nomenclature
- Other information
- The lessons will be given at the Dipartimento di Scienze Farmaceutiche, Via del Liceo, 1; check the room on the website of the Department of Pharmaceutical Sciences : www.dsf.unipg.it
The starting and end of the lessons will be published on the web of the Department. - Learning verification modality
- The student must take an oral exam aimed at verify:.
the knowledge of the structure of the compounds studied, their nomenclature and synthetic strategies. The student should then demonstrate to be able to analyze a class of drugs from a structure-activity-relationship point of view, on the basis of the mechanism of action , therapeutic application, and their side effects. Alternatively, given a pathology, the students should be able to suggest the most appropriate class of drugs with their advantages and disadvantages. All the above knowledge are essential for a graduated students who will work as a pharmacist , but above all for the graduated student who will work as a researcher in a pharmaceutical company, where to design a new entity, it is mandatory to know the state of the art. - Extended program
- Introduction to pharmaceutical chemistry. Drugs in clinical practice: classified by
type, by prescription, and by sales. History of drugs. Definition of
a drug. Sources of drugs. How to identify a hit compound: from
serendipitous discovery to rational design. From hit to lead, to the introduction of
a drug into clinical practice. Chemical-physical properties of a molecule,
relationship between chemical-physical properties and biological activity. Mechanism
of action of drugs. Drug-receptor binding. Various biological targets:
membrane receptors, cytoplasmic receptors, enzymes, nucleic acids. Introduction to
pharmacokinetics: Phase I and II metabolism. Prodrugs. Various classes of
drugs: modulators of the cholinergic system: muscarinic and nicotinic
agonists and antagonists; AchE inhibitors. Drugs of the
adrenergic system: direct and indirect, agonists and antagonists, selective for
alpha or beta receptors. Antihistamines (antiallergic and antiulcer);
Central nervous system drugs: CNS depressants and stimulants.
Opioid analgesics (opioid receptors, opioid peptides, morphine, and
simplified derivatives); anxiolytics (benzodiazepines), sedative-hypnotics
(barbiturates), anticonvulsants (barbiturates, hydantoins, oxazolidinediones,
succinimides, and other more recent derivatives); antipsychotic agents (schizophrenia,
dopaminergic hypothesis), typical neuroleptics (reserpine, phenothiazines,
thioxanthenes, butyrophenones) and atypical neuroleptics (substituted benzamides);
serotonergic
hypothesis (benzoazepine derivatives, SDAs). Antidepressants, depression, monoaminergic hypothesis, MAO inhibitors, tricyclic and atypical antidepressants, SSRIs (selective serotonin reuptake
inhibitors); mood stabilizers.
Nomenclature and synthesis of selected drugs within the various classes. - Obiettivi Agenda 2030 per lo sviluppo sostenibile
- The course aligns with some of the goals of the 2030 Agenda