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Drug Discovery: basic principles


Drug Discovery: basic principles


Academic year 2020/2021

Course ID
BIO0170B Pds 306-TB
Prof.ssa Sonja Visentin (Lecturer)
Modular course
Degree course
[0101M21] Molecular Biotechnology
2nd year
Teaching period
To be defined
Related or integrative
Course disciplinary sector (SSD)
CHIM/08 - chimica farmaceutica
Formal authority
Type of examination
Written and oral
Elements of organic chemistry and biochemistry.
Propedeutic for
This teaching is a point of arrival. It is not propaedeutical.

Sommario del corso


Course objectives

The main objective of the course is to provide students with the basics of drug discovery and understanding the relationship between the chemical structure of molecules and their pharmacological activity. Moreover, the course prefigures to provide the student with a highly professionalized competence of business and national pharmaceutical research centers, on the different aspects of instrumental analysis in the different phases of the discovery, development and production process  of the pharmaceutical industry.


Results of learning outcomes

At the end of the course, students should be able to have learned the various stages that make up the pipeline of drug discovery and understand the chemical and physical properties of the molecules in the pharmaceutical field


Course delivery

The course will be delivered through frontal lectures using the Moodle platform

Lessons: 40 hours

After the recent emergency situation, the teaching will be made compatible with an integrated learning environment in e-learning mode, suitable for face-to-face situations, those in which teaching is provided entirely online and forms of blended teaching.

Depending on the changing situations, the platform course will welcome: lesson materials (video recordings and / or audio presentations); exercises to be carried out online, but also face-to-face; in-depth teaching materials that can be discussed through a forum and / or in the classroom during the lesson-debate. The objective of the learning environment is to create continuity between the different teaching moments and between the different situations (remote activities and face-to-face activities).


Learning assessment methods

The exam is divided in  two parts:

  • writing a scientific article about a drug assigned to each candidate at least 15 days before the examination date, using a track provided by the teacher (max 27/30)
  • Oral exam on the program

The unit of measure: thirty/30

Depending on the recent emergency situation, the exam may be in oral remote (webex) mode.



  • Introduction to drug discovery ; identification of the target and the ligand ; virtual screening ; drug discovery based on fragments ; transformations of lead ; isosterism and bioisosterism ; Introduction to QSAR ; synthesis of peptides and SPPS ; Combinatorial Approach to Drug Discovery ; example of study.
  • Physico-chemical properties of molecules and their influence on the interaction between drugs and their targets :
  • type of bond and their strength, intermolecular forces, ionization, lipophilicity
  • Relevance of the structures of proteins and DNA drug-receptor interaction
  • Principles of Pharmacodynamics Pharmacokinetics ( ADMET )
  • Molecular Descriptors involved in the determination of the ADME profile of potential drugs
  • Principles of Pharmacodynamics Pharmacokinetics ( ADMET )
  • Structure- activity relationship and drug design
  • Drug Discovery for biotechnological drugs
  • Nanotechnology for drug delivery

Suggested readings and bibliography


Burger's Medicinal Chemistry and Drug Discover

Author: Donald Abraham and David Rotella

Publisher: Wiley
ISBN: 978-0-470-27815-4

Pharmaceutical Analysis
Author: David Watson
Publisher: Elsevier
ISBN: 9780702051296



The teaching activity may vary according to the limitations imposed by the current health crisis. In any case, the remote mode is ensured throughout the academic year

Last update: 28/09/2020 15:32
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