Medicinal Chemistry

Objectives

To convoy a multidisciplinary approach of the design and development of drugs. It is expected to highlight the importance of medicinal chemistry in our lives and how several scientific areas are overlaped in medicinal chemistry in order to develop a new drug.

The program describes the molecular  mechanisms by which drugs act in the body, as well as  the steps involved in the discovery of drugs. Examples of optimization of structure-activty relationship will be given.

Selected topics in medicinal chemistry will be covered, such as antibacterial agents, antivirals and others.

General characterization

Code

8889

Credits

6.0

Responsible teacher

Maria Manuel Martinho Sequeira Barata Marques

Hours

Weekly - 3

Total - 50

Teaching language

Português

Prerequisites

The drug and its biological target. Interaction of drugs with biological systems. Drug targets. Pharmacodynamics and pharmacokinetics. Discovery, design, and development of drugs. Search for lead structures. Optimization of interactions with targets. Structure-activity relationship. Optimization of the drug access to the target. Bioassay methods.

The combinatorial approach. Examples of construction of combinatorial libraries.

Selected topics in medicinal chemistry.

Bibliography

INTRODUCTION TO MEDICINAL CHEMISTRY, 4th ed. G.H Patrick, Oxford University Press, Oxford, 2008.

QUÍMICA MEDICINAL. AS BASES MOLECULARES DA AÇÃO DOS FÁRMACOS. E.J. Barreiro, C.A.M. Fraga, ARTMED Ed, Porto Alegre, 2008.

THE ORGANIC CHEMISTRY OF DRUG DESIGN AND DRUG ACTION, 2nd ed., R.B., Silverman, Elsevier Academic Press, Burlington, San Diego, London, 2004.

MOLECULES AND MEDICINE. E.J.Corey, B.Czakó, L Kürti (Eds). J. Wiley & Sons, New Jersy, 2007.

CHEMISTRY AND MEDICINES, AN INTRODUCTORY TEXT. J.R. Hanson RSC Publishing, Cambridge, 2006.

MOLECULES THAT CHANGED THE WORLD. K.C. Nicolaou, T. Montagnon Wiley-VCH, 2007.

THE PRACTICE OF MEDICINAL CHEMISTRY, 3th ed., C.G.Wermuth (Ed), Academic Press, Burlington, San Diego, London, 2008.

Teaching method

Theoretical live classes (PowerPoint).

Some seminars will be given by invited  reserachers on topics related with the program.

The evaluatiion consists of 2 tests (35% + 35%), and 1 highlight (writen + oral) about a drug choosen by the student (30%).

Evaluation method

This discipline contains the following evaluation items:

- 2 TESTS (35% + 35%) - evaluation of theoretical-practical component;

- 1 HIGHLIGHT (30%) (WRITEN + ORAL) - evaluation of the component seminar-type;

The evaluation of the theoretical-practical component (70%) can be improved at the exams season.

Subject matter

Introduction to medicinal chemistry: the drugs and the targets - proteins and enzymes - its structure and function. Interaction of the drugs with biological targtes.

Phramacodynamics and pharmacokinetics.

The discovery of drugs, the design and development of drugs. Finding a lead; Structure-activity relationship. Optimization of the the access to the target. Pre-clinical and clinical tests. Geting a drug to the market.

The program involves some classes on combinatorial chemistry and computacional chemistry that will be given by expert in the field.

Examples of libraries of compiunds and related topics on medicinal chemistry will be given, such as antibacteral agents, antiviral agents, anticancer agenst and others.

Tere will be some seminars given by external researchers working in the field.

Programs

Programs where the course is taught: