Medicinal Chemistry
Code
8889
Academic unit
Faculdade de Ciências e Tecnologia
Department
Departamento de Química
Credits
6.0
Teacher in charge
Pedro Jorge Macedo de Abreu
Weekly hours
3
Total hours
50
Teaching language
Português
Objectives
To convoy a multidisciplinary approach of the design and development of synthetic and natural drugs.
The program describes the molecular basis of drug action in the organism, and the steps involved in the discovery of drugs, featuring several examples of structure-activity optimization of molecules having an effect on target systems.
Main strategies of research of natural product chemistry aiming the discovery of new drugs are highlighted, namely, the combinatorial approach.
Patents of brand name drugs and generics are briefly introduced.
Subject matter
Medicinal plants and their active constituents. Ethnopharmacology. 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. Pro-drugs. Isosteres. Drugs “me-too”. Preclinic and clinic assays. Drug patents. Natural products as source of new drugs. Strategies for lead structure discovery from natural products. Bioguided isolation.
Bioassay methods. Hyphenated analytical tools coupled with bioassays. High Throughput Screening (HTS). The combinatorial approach. Examples of construction of combinatorial libraries. Bioactive molecules from microorganisms. The post-genomic era of natural products. Combinatorial biosynthesis, and precursor directed biosynthesis.
Conferences on Medicinal Chemistry topics.
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 PRACTICE OF MEDICINAL CHEMISTRY, 3th ed., C.G.Wermuth (Ed), Academic Press, Burlington, San Diego, London, 2008.
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.
THE ORGANIC CHEMISTRY OF DRUG DESIGN AND DRUG ACTION, 2nd ed., R.B., Silverman, Elsevier Academic Press, Burlington, San Diego, London, 2004.
MOLECULES THAT CHANGED THE WORLD. K.C. Nicolaou, T. Montagnon Wiley-VCH, 2007.
Teaching method
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Theoretical live classes (PowerPoint). In the coarse of the semester, investigators from the Chemistry Department should be invited to present talks of subjects related with the program of the course. The evaluatiion consists of 2 tests (25% + 25%), and 1 seminar about a drug choosen by the student (50%), which includes a (monography and an oral presntation. |
Evaluation method
2 MINI-TESTS (25% + 25%) + 1 INDIVIDUAL SEMINAR (50%), INCLUDING A SHORT MONOGRAPHY ABOUT A DRUG, AND ORAL PRESENTATION.