| Code |
17258
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| Year |
1
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| Semester |
S2
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| ECTS Credits |
6
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| Workload |
TP(60H)
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| Scientific area |
Biochemistry
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Entry requirements |
Knowledge of General and Organic Chemistry, as well as basic knowledge of Biology and Physiology.
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Learning outcomes |
The Bioactive Compound Development course aims to provide current knowledge on the molecular basis of the discovery, design, development, and action of bioactive compounds, focusing on molecules of interest to human medicine, more specifically:
- To understand the essential physicochemical and structural bases for the rational design and comprehension of the molecular mechanisms of action of active principles;
- To understand current methods and strategies for the discovery and development of prototypes;
- To know how to relate the chemical characteristics of bioactive compounds to their bioavailability and pharmacokinetics;
- To know, interpret, and predict structure-activity relationships in a rational and mechanistic way;
- To know and predict interactions of bioactive compounds with the main biological targets and the underlying molecular mechanisms.
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Syllabus |
Theoretical:
1. Basic concepts in Medicinal Chemistry, classification and nomenclature of bioactive compounds
2. Structural and physicochemical factors of bioactive compounds and their importance in Medicinal Chemistry
3. Discovery, design and development of bioactive compounds – prototype discovery and its modifications, QSAR and CADD
4. Metabolism and chemical mechanisms of bioactivation
5. Prodrugs and delivery systems of bioactive compounds – development, activation and applications
6. Interactions with receptors and design and development of agonist and antagonist agents
7. Enzymes and design and development of enzyme inhibitors
8. Nucleic acids and classes of bioactive compounds that interact with DNA
Practical/Laboratory – problems and/or laboratory studies on:
1. Nomenclature of bioactive compounds
2. Factors affecting the activity of bioactive compounds
3. QSAR and CADD
4. Prediction of xenobiotic metabolism and development of prodrugs
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Main Bibliography |
1. G. L. Patrick, An Introduction to Drug Synthesis, Oxford University Press, 2015;
2. R. B. Silverman, The Organic Chemistry of Drug Design and Drug Action, 2nd Ed., Elsevier Academic Press, 2004;
3. G. L. Patrick, An Introduction to Medicinal Chemistry, 6th Ed., Oxford University Press, 2017;
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. C. Dickson, Medicinal Chemistry Laboratory Manual, CRC Press: Boca Raton, London, New York, Washington DC, 1999;
8. http://old.iupac.org/publications/cd/medicinal_chemistry/
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Teaching Methodologies and Assessment Criteria |
Teaching through theoretical and practical classes, including seminars with a participatory and interactive approach, problem-based learning activities, and laboratory activities.
Course Attendance:
- Attendance is mandatory, with a maximum of 30% unjustified absences from classes without laboratory work.
- Attendance at classes with laboratory activities is mandatory, with only one absence (2 hours) tolerated, but all laboratory work must be completed (laboratory classes will be rescheduled in case of justified absence), and the complete laboratory notebook will be evaluated.
- Evaluation will be continuous, and it is mandatory to complete all evaluations, including the laboratory notebook and the seminar.
The evaluation will include a written exam on theoretical and practical content (60%), a written exam on laboratory activities (20%), laboratory notebook (5%), and a seminar on an article (15%).
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Language |
Portuguese. Tutorial support is available in English.
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