Teacher(s)

Frédérick Raphaël; Lambert Didier; Muccioli Giulio (coordinator);

Language

French

Main themes

The purpose of this medicinal chemistry course is to enable the student to understand, via selected examples, the different strategies used in medicinal chemistry to discover and optimize a drug. We will cover topics ranging from the choice of the therapeutic target of interest to the marketed molecule, via the discovery of potentially interesting molecules (a.k.a. 'hits') and their optimization into 'leads'.
It will also discuss aspects of the interaction between molecules and targets to emphasize their importance in the action of drugs, as well as the strategies of the medicinal chemist to modulate the passage of the blood-brain barrier. 

Aims

At the end of this learning unit, the student is able to :
1	- Give to the student the appropriate knowledge: on the key steps leading to the discovery and development of a drug on how to integrate the specific knowledge in chemistry, pharmaceutical chemistry, pharmacology, and toxicology into the process of discovery, evaluation and development of new drugs  The contribution of this Teaching Unit to the development and command of the skills and learning outcomes of the programme(s) can be accessed at the end of this sheet, in the section entitled 'Programmes/courses offering this Teaching Unit'. - Give to the student the appropriate knowledge: on the key steps leading to the discovery and development of a drug on how to integrate the specific knowledge in chemistry, pharmaceutical chemistry, pharmacology, and toxicology into the process of discovery, evaluation and development of new drugs  The contribution of this Teaching Unit to the development and command of the skills and learning outcomes of the programme(s) can be accessed at the end of this sheet, in the section entitled 'Programmes/courses offering this Teaching Unit'.

Content

This course addresses important concepts in the context of "drug discovery" for pharmaceutical sciences undergraduate students. While the more specialized notions are discussed in elective courses, this course will give a glimpse of the methodologies used to develop, characterize, and improve a drug.
Among the elements discussed, we can mention:
1.      Target identification by the « omic » approaches
2.      Orphan GPCRs as drug targets
3.      Real world Drug Discovery
4.      Medicinal chemistry in the academic world
5.      Structure-based and fragment-based drug design
6.      Lead-like properties
7.      BBB crossing by drugs: from evaluation to optimization and prodrug strategies
8.      From in-vitro to in-vivo and to the patient
9.      Medicinal chemistry in the Pharma industry
10.  Big size drugs

Teaching methods

Due to the COVID-19 crisis, the information in this section is particularly likely to change.

Courses will be given by experts in the field, including from the pharma industry

Evaluation methods

Due to the COVID-19 crisis, the information in this section is particularly likely to change.

Evaluation by a written exam

Online resources

An adapted version of the material presented during the lessons is available on the "moodle" platform.

Teaching materials

• une version des supports présentés est disponible sur moodle

Faculty or entity

FARM