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Drug Development and Synthesis

Code 13683
Year 2
Semester S2
ECTS Credits 6
Workload PL(30H)/T(30H)
Scientific area Ciências Farmacêuticas
Entry requirements To have thorough knowledge of General and Organic Chemistry and basic knowledge of Biology and Physiology.
Learning outcomes The Curricular Unit “Drug Development and Synthesis” aims to provide current knowledge on the molecular basis of drug discovery, development and synthesis, more specifically:
-to know the physicochemical and structural basis to the rational development of drugs;
-to know the current methods and strategies for leads discovery and development and for obtaining and interpreting structure-activity data;
-to understand the role of organic chemistry in drug development and preparation;
-to know the main semi-synthetic and synthetic approaches in the preparation of the most relevant drug classes.
Syllabus --Theoretical:
1. Basic concepts in pharmaceutical chemistry, drug classification and nomenclature
2. Structural and physicochemical characteristics most relevant in drug development and action
3. Drug discovery, design and development – lead discovery and its modifications, qualitative and quantitative structure-activity relationships and computational design.
4. Importance of organic synthesis in obtaining pharmacologically active molecules
5. Targeted- and diversity-oriented synthesis and high throughput methodologies
6. Introduction to retrossynthetic analysis, protecting groups and selectivity
7. Semi-synthetic and synthetic approaches in the preparation of the most relevant drug classes.
--Practical/Laboratory - problem solving and laboratory studies on:
1. Nomenclature and synthesis of drugs
2. Factors Affecting Drug Activity
3. Computer-Aided Drug Development
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 Síntesis de Fármacos, Editorial Sintesis, 2002;
7. A. Delgado, C. Minguillón, J. Joglar, Introductión a la Química Terapéutica, 2ª Ed., Diaz de Santos, 2003;
8. C. Dickson, Medicinal Chemistry Laboratory Manual, CRC Press: Boca Raton, London, New York, Washington DC, 1999;
Teaching Methodologies and Assessment Criteria Teaching through lectures (T) (seminars; participatory and interactive approach), and theoretical-practical (problem-based learning) and laboratory (PL). The learning activity will focus significantly on the student.

Continuous assessment (required):
A) Theoretical and theoretical-practical component (65%):
-3 frequencies (21% + 22% + 22%)
B) Laboratory component (35%):
-attitudes of each student in classes (5%)
-laboratory notebook (5%)
-individual test on practical subjects (25%)
It is not necessary to attent the final exam if:
-final grade of the theoretical part is equal or higher than 9,5 values,
-final grade of the practical / laboratory part is equal or higher than 9.5 values and
-average of both components is equal or higher than 9.5 values

Final exam:
-includes all theoretical / theoretical-practical (65%) and laboratory (35%) contents
Language Portuguese. Tutorial support is available in English.
Last updated on: 2024-02-26

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