2017/2018

2019/2020

DM270

CHIM/08 (PHARMACEUTICAL CHEMISTRY)

DEPARTMENT OF DRUGS SCIENCES

MEDICINAL CHEMISTRY AND PHARMACEUTICAL TECHNOLOGY

PERCORSO COMUNE

3°

1st semester (01/10/2019 - 31/01/2020)

9

72 lesson hours

Italian

WRITTEN AND ORAL TEST

MASSOLINI GABRIELLA (titolare) - 8 ECTS
BAVARO TEODORA - 1 ECTS

The student should have adequate knowledge of general and inorganic chemistry (equilibrium in solution), organic chemistry (funtional Group reactivity), basic knowledge of anatomy, physiology, biochemistry and biology.

Medicinal Chemistry is focused on the discovery and development of biologically active agents with potential therapeutic
application.
The course provides the basic knowledge of medicinal chemistry to understand the the
structure-activity relationships (SAR) of drugs. The student will be able to correlate chemical characteristics of active molecules to the
adsorption, distribution, metabolism, excretion and toxicity. The molecular modifications of lead compounds can be
discussed together with the strategies for the drug discovery.
At the end of the course, the student will know the main classes of drugs that interact with neurotransmitter receptors, intracellular receptors, enzymes and ion channels, and, for each class of drugs, the most representative components in use, their chemical-physical and biological properties and their structure-activity relationships.

General Medicinal Chemistry Historical perspective of medicinal chemistry. Drug design and relationship
between functional groups and activity. Mechanisms of action of drugs. Physicochemical and biopharmaceutical
properties of bioactive molecules. Pharmacokinetic aspects. Medicinal chemistry of molecular targets
Receptors as targets : general aspects and perspectives. Metabotropic receptors as drug targets: cholinergic and
adrenergic receptors and drugs active on the cholinergic and adrenergic neurotransmission; serotonin receptors and
drugs acting on serotonergic neurotransmission; histamine receptors and related drugs. Channel receptors as drug
targets: amino acid neurotransmitters in the central nervous system; nicotinic drugs. Enzymes as drug targets: inhibitors
of phosphodiesterase, cholinesterase, ACE, HMG CoA reductase, cyclooxygenase inhibitors and NSAIDs. Ion channels
as drug targets: inhibitors of calcium channels, potassium, sodium and chlorine. Local anesthetics. Part C - Therapeutic
Medicinal Chemistry
DRUGS ACTING on the CENTRAL NERVOUS SYSTEM
General anesthetics. Sedative hypnotics. Anticonvulsant drugs. Antidepressants. Psychotherapeutic drugs: agents
antipsychotics and anxiolytics. Hallucinogens, stimulants and drugs of abuse related. Opioid analgesics. Drugs used in
treatment of neurodegenerative diseases: antiparkinsonian agents and antispasmodic; Alzheimer's disease.
DRUGS ACTING on the CARDIOVASCULAR AND RESPIRATORY SYSTEMS
Cardiac drugs: antianginal, antiarrhythmic agents. Antihypertensives, diuretics. Antiplatelet agents,anticoagulants and fibrinolytics. Asthma and antitussives.
DRUG ACTING on the GASTROENTERIC SYSTEM
Anti-ulcer, anti-diarrheal.

The course is organized in frontal lectures through PowerPoint presentations and interactive lessons through the use of the Kiro UniPV multimedia platform (University of Pavia's didactic portal). Some arguments will be given to the students for preparing an oral reports

Gasco-Gualtieri-Melchiorre “Chimica Farmaceutica” Casa Editrice Ambrosiana Edizione 2015
Lemke & Williams “Foye’s Principi di Chimica Farmaceutica”, Piccin. Quinta Ed Italiana, 2010
Patrick GL “Introduzione alla Chimica farmaceutica” Edises. Seconda Ed Italiana, 2010

The exam is made up of one test at the end of the lessons or a final exam, in both cases the exam will be written with multiple answer questions and open questions. The student will need to identify the structure of a drug, describe the structure-activity relationships, identify the mechanism of action, metabolism, or pathology for which the molecule is indicated.
The overall written test consists of 12 questions (score 3 or 4 points), each with 3/4 possible answers and with more than one answer correct, and two open questions (score 7 points), to be completed in 90 minutes.
An oral test is foreseen to evaluate the ability to discuss the content of the course and to achieve the course objectives.
Evaluation procedures are appropriate to expected learning outcomes, and students are informed about the profit verification strategy, the methods adopted, the criteria applied in the assessment, and the consequences of all possible relevant events for the assessment ( Absences, sanctions for misconduct, etc.).

The exam is made up of one test at the end of the lessons or a final exam, in both cases the exam will be written with multiple answer questions and open questions. The student will need to identify the structure of a drug, describe the structure-activity relationships, identify the mechanism of action, metabolism, or pathology for which the molecule is indicated.
The overall written test consists of 12 questions (score 3 or 4 points), each with 3/4 possible answers and with more than one answer correct, and two open questions (score 7 points), to be completed in 90 minutes.
An oral test is foreseen to evaluate the ability to discuss the content of the course and to achieve the course objectives.
Evaluation procedures are appropriate to expected learning outcomes, and students are informed about the profit verification strategy, the methods adopted, the criteria applied in the assessment, and the consequences of all possible relevant events for the assessment ( Absences, sanctions for misconduct, etc.).