Strategies in Drug Discovery

Recommended Prerequisites

The recommended prerequisites include what is taught in the 1 st cycle courses in the area of Medicinal Chemistry, Chemical Sciences, Biochemistry, Bioanalytical and Medical Sciences, and other courses considered appropriate by the Master Coordination Board.

Teaching Methods

In the theoretical classes, the concepts and methods for strategies in drug discovery will be delivered and representative examples, taken from recent literature, will illustrate them.

The theoretical-practical classes will address the presentation and discussion of case studies on the subject.

The seminars will be on complementary research areas to the subjects presented and discussed in the classes.

The synthesis work will consist in a state of the art of a scientific theme.

The exam is designed to check the acquired knowledge by the students.

Learning Outcomes

This curricular unit aims to guide the students on the strategies in use for drug discovery. The fundamental concepts and methods in drug discovery will be outlined.
Competencies
•    Advanced knowledge in drug discovery
•    Skills in strategies to discover new hits
•     Knowledge on drug metabolism and structural alerts for toxicity
•    Critical view on scientific information to develop a research project
•    Ability to integrate a multidisciplinary research group for drug discovery

Work Placement(s)

No

Syllabus

1. Hit to lead process in drug discovery

2. High-throughput screening and compound collection enhancement

3. Lead-likeness and drug-likeness

4. Conformational restriction and optimization of lead molecules

5. Discovery of multi-target molecules

6. Metabolism and structural marks for toxicity

7. Examples on drug discovery, namely for central nervous system diseases, metabolic disorders, in oncology and for infectious diseases.

Head Lecturer(s)

Jorge António Ribeiro Salvador

Assessment Methods

Assessment
Report of a seminar or field trip: 10.0%
Problem solving report: 20.0%
Synthesis work: 20.0%
Exam: 50.0%

Bibliography

Abraham D J, Rotella D P, Burger’s Medicinal Chemistry, Drug Discovery and Development , Wiley, 7th Ed., 2010

Chorghade M S, Drug Discovery and Development, Wiley, 1st Ed., 2006

Nature Reviews Drug Discovery