Drug Discovery, Design and Development
The objective of this curricular unit (CU) is to contribute to the formation of future researchers or pharmaceutical industry professionals, equipped to understand and act upon the several stages of the creation of an active principle, its transformation into a drug and its introduction to the market as an efficient and safe medicine.
At the end of this CU the student must grasp and be able to articulate the following topics:
- Processes of identification and discovery of new active principles;
- Methodologies for the design and optimization of the active principles relative to their therapeutic target;
- Methods to optimize administration, distribution and delivery of the active principle in vivo;
Stages and requirements of the process of bringing a drug to the market.
Maria Rita Mendes Bordalo Ventura Centeno Lima
Weekly - 2
Total - 24
This CU aims at the preparation of scientists motivated to work in the pharmaceutical industry, in research or in entrepreneurial projects in the area of drug discovery and development. Obviously, this capability requires fundamental knowledge in the areas of Chemistry and Biology that lie beyond those dealt with in this CU. In particular, it is fundamental to acquire prior knowledge of the fundamentals of chemical synthesis as well as those regarding the biochemistry of disease and the tools of Bioinformatics which structure the rationale for molecule search and design in the chemical space.
Graham L. Patrick, An Introduction to Medicinal Chemistry
Gareth Thomas, Fundamentals of Medicinal Chemistry
The Practice of Medicinal Chemistry
Camille G. Wermuth, (Ed) The Practice of Medicinal Chemistry
B. Silverman, The Organic Chemistry of Drug Design and Drug Action
Drug Discovery Today, Elsevier periodical with extensive discussions, updates and case studies in Drug Discovery and Development.
Presential teaching will be made through regular lectures and tutorials as well as through seminars delivered by invited specialists on selected topics or relevant Case Studies.
The final evaluation will comprise one written test to be done during the semester (60%), and a final seminar (with public discussion) on a theme to be selected from a previously announced set (40%).
Drugs and drug targets: Introduction
Proteins as drug targets
Enzymes as drug targets
Receptors as drug targets
Nucleic Acids as drug targets
Other molecular drug targets: lipids, carbohydrates, etc...
Drug discovery, Design and Development
Finding a lead compound
Develop a bioassay
Design of the Lead compound
optimize interactions with the Target: (SAR; pharmacophore)
optimizing the drug
optimizing access to the target
Problems of Formulation and Drug Delivery
methods to prepare water soluble compounds
solubilizing drugs in organic solventes, micelles or coloidal dispersions
solubilization with cyclodextrins
Bringing Drugs to the Market
Selected Topics (e.g. antibacterials, anti-cancer drugs) and Case Studies.
Programs where the course is taught: