Fundamentals of Medicinal Chemistry

Year
1
Academic year
2016-2017
Code
02031627
Subject Area
Medicinal Chemistry
Language of Instruction
Portuguese
Other Languages of Instruction
English
Mode of Delivery
Face-to-face
Duration
SEMESTRIAL
ECTS Credits
6.0
Type
Elective
Level
Non Degree Course

Recommended Prerequisites

Not applicable.

Teaching Methods

Expositive classes and seminars delivered by specialists with students interaction according to what is expected at the PhD level.

Learning Outcomes

Provides a common scientific background and key concepts in drug discovery to all graduate students.

Work Placement(s)

No

Syllabus

1. Administration, biodistribution and fundamental pharmacokinetics

2.Lead validation

3. Drug targets. enzymes, receptors, nucleic acids

4. The prodrug concept - application in drug design. Soft drugs. Drug targeting

5. Hit discovery strategies.

6. Chemical libraries

7. Bridging drug synthesis to biological testing

8. Targets for drug development in ageing and age-related neurodegenerative disorders

9. Metabolism

Head Lecturer(s)

Luís Guilherme da Silva Arnaut Moreira

Assessment Methods

Assessment
Exam: 100.0%

Bibliography

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M. R. Prausnitz, R. Langer, Transdermal Drug Delivery. Nature Biotech., 2008, 26, 1261-1268.

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Antonia F. Stepan, Daniel P. Walker, Jonathan Bauman, David A. Price, Thomas A. Baillie, Amit S. Kalgutkar, and Michael D. Aleo, Structural Alert/Reactive Metabolite Concept as Applied in Medicinal Chemistry to Mitigate the Risk of Idiosyncratic Drug Toxicity: A Perspective Based on the Critical Examination of Trends in the Top 200 Drugs Marketed in the United States, Chem. Res. Toxicol., 2011, 24 (9), 1345–1410.

http://dx.doi.org/10.1021/tx200168d

Eric A. G. Blomme and Yvonne Will, Toxicology Strategies for Drug Discovery: Present and Future, Chem. Res. Toxicol., Article ASAP, Publication Date (Web): November 20, 2015

http://dx.doi.org/10.1021/acs.chemrestox.5b00407

Yankner BA, Lu T, Loerch P. The aging brain. Annu Rev Pathol. 2008;3:41-66.

Raskin J, Cummings J, Hardy J, Schuh K, Dean RA. Neurobiology of Alzheimer's disease: integrated molecular, physiological, anatomical, biomarker, and cognitive dimensions. Curr Alzheimer Res. 2015, 12:712-22.

R.B. Silverman and M.W. Holladay, The Organic Chemistry of Drug Design and Drug Action, 2014, 3rd edition, Elsevier Academic Press.

E.H. Kerns and L. Di, Drug-like properties: Concepts, Structure Design and Methods – from ADME to Toxicity  Optimization, 2008, Elsevier Academic Press.