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Medicinal Chemistry I

Code 10258
Year 3
Semester S1
ECTS Credits 6
Workload PL(30H)/T(30H)
Scientific area Química Medicinal
Mode of delivery Face to face classes and in the form of self-learning by the student.
Work placements Not planned.
Learning outcomes The Medicinal Chemistry I Curricular Unit aims to provide current knowledge about the molecular basis of drug discovery, design and development and molecular actions. At the end of this Curricular Unit, the student should be able:
-to know the chemical and structural characteristics critical to perform the rational drug design and to understand the molecular mechanisms of drug action;
-to know and apply the current methods and strategies for the discovery and development of leads;
-to predict the effects of the chemical characteristics of drugs in their bioavailability and pharmacokinetics;
-to evaluate, interpret and predict structure-activity relationships in a rational and mechanistic way;
-to understand and to predict drug interactions with key biological targets and the molecular mechanisms underlying.
Syllabus Theoretical:
1. Basic concepts in Medicinal Chemistry, classification and nomenclature of drugs
2. Structural factors and physico-chemical characteristics of drugs and their importance in Medicinal Chemistry
3. Drug discovery, design and development - the discovery of the prototype and its modifications, QSAR and CADD
4. Drug metabolism and chemical mechanisms of bioactivation
5. Prodrugs and drug delivery systems - development, activation and applications
6. Drug-receptor interactions and drug design and development of agonists and antagonists
7. Enzymes and design and development of enzyme inhibitors
8. Nucleic acids and classes of drugs that interact with DNA

Practical / Lab - problem solving and laboratory studies on:
1. Naming of drugs
2. Factors affecting the activity of drugs
3. QSAR and computational analysis of 3D structures of a drug-receptor complex
4. Prediction of xenobiotic metabolism and development of prodrugs
Main Bibliography Main bibliography:
1. R. B. Silverman, The Organic Chemistry of Drug Design and Drug Action, 2nd Ed., Elsevier Academic Press, 2004;
2. G. L. Patrick, An Introduction to Medicinal Chemistry, 4th Ed., Oxford University Press, 2010;
3. C. Avendaño, Introductión a la Química Farmacéutica, 2ª Ed., Mc.Graw-Hill, 2001;

1. T. L. Lemke, D. A. Williams, FOYE´s Principles of Medicinal Chemistry, 6th Ed., Lippincort Williams & Wilkins, 2008;
2. C. Dickson, Medicinal Chemistry Laboratory Manual, CRC Press: Boca Raton, London, New York, Washington DC, 1999;
Language Portuguese. Tutorial support is available in English.
Last updated on: 2012-05-21

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