Medicinal Chemistry 1

A.Y. 2019/2020
10
Max ECTS
80
Overall hours
SSD
CHIM/08
Language
Italian
Learning objectives
The lectures are aimed at providing the student with background knowledge and understating
- of how drugs interacts with their biological targets
- of how drugs get to their targets (ADMET)
- of the main principles of drug design and development
- of the issues in drug design (SAR and QSAR)
- of some classes of drugs, such as antibacterial, antiprotozoal, antiviral and anticancer agents.
Expected learning outcomes
At the end of the course, the student is expected:
- to know the principles and the strategies applied in the rational drug design;
- to critically evaluate the chemico-physical properties and the structure-activity relationships for the considered classes of drugs
- to gain the theoretical bases to understand how the pharmacokinetic profile influences the activity of a given drug
- to reach lifelong learning skills involving a multifaceted knowledgebase on how the chemical properties impact on drug activity. These skills will be useful for further student's personal study and will allow a proper evaluation of the new drugs that will reach the market.
Course syllabus and organization

Linea AL

Responsible
Lesson period
year
Course syllabus
Introduction to medicinal chemistry
Drug discovery and development
Biotechnologies in drug discovery and development
Action mechanism of drugs
Molecular target of drugs
Receptors as drug targets
Enzymes as drug targets
Drug design and development
Lead compounds in drug discovery
Structure activity relationship (SAR)
The pharmacophore
Isostey and bioisostery
Pharmacokinetics
Prodrugs
Quantitative structure activity relationship (QSAR)

Antibacterial agents
Antibiotics
Antimycobacterial agents
Antiprotozoarian agents
Ectoparasiticides
Antihelminthics
Antimycotic agents
Antiviral agents
Anticancer agents
Insulin, glucagon and hypoglycemic drugs
Prerequisites for admission
To conveniently attend the lessons, the student should possess basic knowledge of organic chemisty, biology and physiology
Teaching methods
Traditional lessons supported by slides (available in Ariel)
Teaching Resources
· G. L. Patrick: an introduction to Medicinal Chemistry. 5th Ed. - Oxford University Press (2013).
ISBN: 978-0-19-969739-7.
· G. L. Patrick: Introduzione alla Chimica Farmaceutica, II Ed. - EdiSES - Napoli (2010).
ISBN: 978-88-7959-663-3.

· T. L. Lemke, D. A. Williams: Foye's Principles of Medicinal Chemistry, 7th Ed. Lippincott Williams &Wilkins. (2013). ISBN: 978-1-4511-7572-1.

· D. A. Williams, T. L. Lemke: "Foye's Principi di Chimica Farmaceutica" PICCIN, Padova, (2010). ISBN: 978-88-299-2034-1.
· Lessons slides del corso (Ariel)
Assessment methods and Criteria
The final written exam has the following characteristics:

It includes (i) open questions (short answers are required in the prefixed number of lines reported in the exam format) and (ii) multiple choice questions dealing with all topics covered by the course by which the student should demonstrate his retention and understanding as well as his capacity to discuss the key concepts of each topic. The mark of the exam will be rapidly recoded and the student could accept or neglect this within the provided deadline. Before this deadline, a meeting will be scheduled during which the students can analyze and discuss the results of their exam.

During a solar year, there will be seven exams and the students can take consecutive exams without any constraining.

The students, who regularly attend the lessons, can also take two partial written tests concerning the program covered during the first and the second semester, respectively. To be admitted to the second partial test, the student must reach at least a mark of 15/30 in the first test. If not, the student has to take the final exam or to wait for partial tests of the next academic year.
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor: Pallavicini Marco

Linea MZ

Responsible
Lesson period
year
Course syllabus
General topics
Introduction to the medicinal chemistry
The drug discovery e development process
The three phases of drug action
Pharmaceutical phase
Pharmacokinetic Phase
Drug metabolism and toxicity
Pharmacodynamic Phase: mechanism of action
Thermodynamics of ligand binding
Rational design of a new drug: basic principles
The role of conformational and configurational effects
The concept of isosterism and bioisosterism
Structure activity relationships
Quantitative Structure activity relationships (QSAR)
Molecular descriptors: focus on lipophilicity
Structure-based and ligand-based drug design

Systematic topics
Disinfectants and antiseptics
Synthetic antibacterial drugs
Antibiotics
Antimycobacterial drugs
Pesticides
Antimalarial drugs
Antiviral drugs
Anticancer drugs
Prerequisites for admission
To conveniently attend the lessons, the student should possess basic knowledge of organic chemisty, biology and physiology.
Teaching methods
The course covers two semesters and comprises 10 CFU (80 hours) of frontal lessons in classroom.
Teaching Resources
For all topics covered during the course, the slides will be provided in the course website (https://gvistolicft1.ariel.ctu.unimi.it/v5/Home). To delve into the covered topics the following textbooks are suggested:
1. G. L. Patrick: an introduction to Medicinal Chemistry. (Last edition) - Oxford University Press.
2. L. Lemke, D. A. Williams: Foye's Principles of Medicinal Chemistry, (Last Edition) Ed. Lippincott Williams &Wilkins.
Assessment methods and Criteria
The final written exam with marks expressed out of thirty has the following characteristics:
It includes open questions dealing with all topics covered by the course by which the student should demonstrate his knowledge and understanding as well as his capacity to properly discuss the key concepts of each topic. The mark of the exam will be rapidly recorded and the student could accept or neglect it within the provided deadline. Before this deadline, a meeting will be scheduled during which the student can analyze and discuss the result of his exam.
There will be seven exams per year and the student can take consecutive exams without any constrain.
The student, which regularly attend the lessons, could also take two partial written tests concerning the topics covered during the first and the second semester, respectively. To be admitted to the second partial test, the student must reach at least a mark of 15/30 in the first test. If not, the student has to take the final exam or to wait for the partial tests of the next academic year.
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor: Vistoli Giulio