Unit MEDICINAL CHEMISTRY I
- Course
- Chemistry and technology of drugs
- Study-unit Code
- 65903809
- Curriculum
- In all curricula
- Teacher
- Oriana Tabarrini
- Teachers
-
- Oriana Tabarrini
- Andrea Astolfi
- Hours
- 72 ore - Oriana Tabarrini
- 6 ore - Andrea Astolfi
- CFU
- 9
- Course Regulation
- Coorte 2020
- Offered
- 2022/23
- Learning activities
- Caratterizzante
- Area
- Discipline chimiche, farmaceutiche e tecnologiche
- Academic discipline
- 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 two tests: a preliminary written test, and then an oral exam.
The written test is aimed at verifying the knowledge of the structure of the compounds studied, their nomenclature and synthetic strategies. On the other hand, the oral exam will verify the general knowledge of the student on medicinal chemistry. The student should 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 the medicinal chemistry. Definition of drug. Sources of drugs. Different ways to the identification of hit compounds: from serendipity to rational design. From hit to lead, to the introduction in therapy. Classification of drugs. Chemical-physical properties of a compound, structure-activity relationship; Mechanism of action of drugs. Drug-receptor interactions. Various drug targets: membrane receptors, cytoplasmatic receptors, enzymes, nucleic acids. Pharmacokinetics: absorbtion and metabolism. Prodrugs. Various class of drugs: modulators of colinergic system : muscarinics and nicotinics agonists and antagonists; AchE inhibitors. Drugs acting on adrenergic system: direct and indirect drugs, agonist and antagonists, comppounds selective for receptors alfa and or beta. Antiistaminic drugs (antillergic and antiulcer). Drugs acting on SNC: stimulants and depressant.
Analgesic narcotics, (oppioid receptors, peptide oppioid, morphine and semplified derivatives); ansiolitics, sedative-hypnotics; anticonvulsants (barbiturates, hydantoins, ossazolidindions and other newer derivatives ) antipsychotic agents (schizophrenia, a hypothesis dopaninergic: typical neuroleptics (reserpine, phenothiazines, thioxanthenes, butyrrophenones) and atypical (substituted benzamides); serotonin hypothesis: benzoazepinic derivatives, SDAS)
Antidepressants (depression, monoaminergic hypothesis, timeretic drugs (MAO inhibitors) and timolettics: nonselective (tricyclic and atypical) and SSRIs (selective serotonin reuptake inhibitors), mood stabilizers); drugs for the symptomatic treatment of Parkinson's disease (dopaminergic therapy, antihistaminic and anticholinergic); drugs to treat ulcers
antiemetic agents (causes of vomiting, various classes; emetics), purgatives and laxatives.
Nomenclature and synthesis of some drugs, selected among the various classes of therapeutic compounds.