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Molecular Basis of Drug Action

Code 13685
Year 3
Semester A1
ECTS Credits 8
Workload PL(15H)/T(30H)/TP(30H)
Scientific area Ciências Farmacêuticas
Entry requirements To have knowledge on Organic Chemistry, Drug Development, Physiopathology and Pharmacology.
Learning outcomes The Curricular Unit (UC) “Molecular Basis of Drug Action” aims to provide current knowledge about chemical structures and their relationship with the molecular mechanisms of pharmacological action and pharmacokinetic aspects of the most used drug families in clinical practice. Thus, it is expected that the student can relate the chemical and structural characteristics of drugs with their general trajectory in the organism and their molecular activity and knows and can rationally and mechanistically interpret structure-activity relationships. This course also aims to address the discovery and development and the general methods of obtaining and quality control of representative drug classes.
Syllabus Theoretical:
A) Introduction to the general molecular basis of drug action:
1. Development of receptor agonists and antagonists, enzyme inhibitors and nucleic acid interacting agents
2. General relationship between drug structure and pharmacokinetics
3. Drug metabolism, chemical mechanisms of bioactivation and prodrugs
B) For the major drug families of clinical interest, address:
1. Structures, nomenclature and main physicochemical properties
2. Discovery, development and general processes for their obtention
3. Molecular mechanisms of pharmacological action
4. Structure-activity relationships
5. Physico-chemical and structural aspects conditioning pharmacokinetics
Practical / Laboratory:
1. Prediction of drug metabolism and prodrug development
2. Obtention of relevant drugs and / or their intermediates
3. Pharmaceutical and pharmacopoeial drugs analysis
Main Bibliography 1. T. L. Lemke, D. A. Williams, FOYE´s Principles of Medicinal Chemistry, 7th Ed., Lippincort Williams & Wilkins, 2013;
2. G. L. Patrick, An Introduction to Medicinal Chemistry, 4th Ed., Oxford University Press, 2010;
3. R. B. Silverman, The Organic Chemistry of Drug Design and Drug Action, 2nd Ed., Elsevier Academic Press, 2004;
4. C. Avendaño, Introductión a la Química Farmacéutica, 2ª Ed., Mc.Graw-Hill, 2001;
5. T. Nogrady, D. F. Weaver, Medicinal Chemistry – A Molecular and Biochemical Approach, 3rd Ed., Oxford University Press, 2005;
6. A. Delgado, C. Minguillón, J. Joglar, Introductión a la Química Terapéutica, 2ª Ed., Diaz de Santos, 2003;
7. A. Delgado, C. Minguillón, J. Joglar, Introductión a la Síntesis de Fármacos, Editorial Sintesis, 2002;
8. C. Dickson, Medicinal Chemistry Laboratory Manual, CRC Press: Boca Raton, London, New York, Washington DC, 1999;
9. http://old.iupac.org/publications/cd/medicinal_chemistry/
Language Portuguese. Tutorial support is available in English.
Last updated on: 2021-06-10

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