Identifying Data 2019/20
Subject (*) Medicinal Chemistry Code 610G01040
Study programme
Grao en Química
Descriptors Cycle Period Year Type Credits
Graduate 2nd four-month period
Fourth Optional 4.5
Language
Spanish
Teaching method Face-to-face
Prerequisites
Department Química
Coordinador
García Romero, Marcos Daniel
E-mail
marcos.garcia1@udc.es
Lecturers
García Romero, Marcos Daniel
E-mail
marcos.garcia1@udc.es
Web
General description Nesta materia ofértase un curso introductorio de Química Médica no que se abordan conceptos básicos relacionados coa estrutura e actividade de fármacos, mecanismos de acción, metabolismo, así como as principais estratexias no deseño e síntese.

Study programme competencies
Code Study programme competences
A1 Ability to use chemistry terminology, nomenclature, conventions and units
A9 Knowledge of structural characteristics of chemical and stereochemical compounds, and basic methods of structural analysis and research
A10 Knowledge of chemical kinetics, catalysis and reaction mechanisms
A13 Understanding of chemistry of main biological processes
A14 Ability to demonstrate knowledge and understanding of concepts, principles and theories in chemistry
A15 Ability to recognise and analyse new problems and develop solution strategies
A16 Ability to source, assess and apply technical bibliographical information and data relating to chemistry
A17 Ability to work safely in a chemistry laboratory (handling of materials, disposal of waste)
A18 Risk management in relation to use of chemical substances and laboratory procedures
A19 Ability to follow standard procedures and handle scientific equipment
A20 Ability to interpret data resulting from laboratory observation and measurement
A21 Understanding of qualitative and quantitative aspects of chemical problems
A22 Ability to plan, design and develop projects and experiments
A23 Critical standards of excellence in experimental technique and analysis
A24 Ability to explain chemical processes and phenomena clearly and simply
A25 Ability to recognise and analyse link between chemistry and other disciplines, and presence of chemical processes in everyday life
A26 Ability to follow standard laboratory procedures in relation to analysis and synthesis of organic and inorganic systems
B1 Learning to learn
B2 Effective problem solving
B3 Application of logical, critical, creative thinking
B4 Working independently on own initiative
B6 Ethical, responsible, civic-minded professionalism
B7 Effective workplace communication
C1 Ability to express oneself accurately in the official languages of Galicia (oral and in written)
C2 Oral and written proficiency in a foreign language
C3 Ability to use basic information and communications technology (ICT) tools for professional purposes and learning throughout life
C4 Self-development as an open, educated, critical, engaged, democratic, socially responsible citizen, equipped to analyse reality, diagnose problems, and formulate and implement informed solutions for the common good
C6 Ability to assess critically the knowledge, technology and information available for problem solving
C7 Acceptance as a professional and as a citizen of importance of lifelong learning
C8 Understanding role of research, innovation and technology in socio-economic and cultural development

Learning aims
Learning outcomes Study programme competences
Know the structure and mode of action of drugs and the relationship with biological activity A1
A9
A10
A13
A14
A15
A16
A21
A24
A25
B1
B2
B3
B4
B6
B7
C1
C2
C3
C4
C6
C7
C8
Know basic principles and strategies used to design and synthesized drugs. A1
A9
A10
A13
A14
A15
A16
A17
A18
A19
A20
A21
A22
A23
A24
A25
A26
B1
B2
B3
B4
B6
B7
C1
C2
C3
C4
C6
C7
C8
Know the impact of drugs and the pharmaceutical companies in the society. A13
A14
A16
A24
A25
B1
B3
B4
B6
B7
C1
C3
C6
C7
C8
The students should be able to identify apropriate information on the scientific literature, assess their responsibility in the management of information and knowledge in the field of Industrial Chemistry and the Chemical Research, use scientific terminology and appreciate the value of quality and continuous improvement A14
A15
A16
A22
A24
A25
B1
B2
B3
B4
B6
C1
C2
C3
C4
C6
C7
C8

Contents
Topic Sub-topic
Chapter 1. Basic principles in Medicinal Chemistry 1.1 Medicinal Chemistry : definition and basic concepts
1.2 Historical Perspective .
1.3 Pharmacokinetics and Pharmacodynamics
1.4 Drug Discovery
1.5 Drugs: nomenclature and classification
Chapter 2. Molecular basis on pharmacological activity:
Pharmacodynamics
2.1 Drug-receptor interactions . Molecular topology and biological activity
2.2 Proteins: structure and function. Protein Interactions
2.3 Enzymes: enzymatic catalysis. Michaelis - Menten equation . Enzyme inhibition : Types
2.5 Cell receptors: structure and classification .
2.6 Nucleic Acids . Structure and functions. Drug interactions with nucleic acids
2.7 Interactions with lipid and carbohydrate
Chapter 3. Phramacokinetics 3.1 ADME processes.
3.2 Absorption of drugs. Modes of administration . Physicochemical properties of drugs : Lipinsky rules . Bioavailability .
3.3 Distribution of drugs. Blood : composition and properties. Removal rate . Mid life. Volume of distribution
3.4 Drug metabolism : metabolism in phase I and phase II
3.5 Elimination of drugs.
Chapter 5. Drug discovery 4.1 Steps in drug discovery. Biological target vs Phenotypic approach. Structural diversity. Chemical space. Drug binding energy. High Throughput Screening ( HTS ). Chemical libraries: combinatorial chemistry , parallel synthesis , solid phase synthesis
4.2 Strategies in drug discovery (lead discovery) . Screening modes . Drug screening methods . Drug Design
4.3 Optimization of drugs (lead optimization) . Structure- actividadIdentificación pharmacophore . Pharmacomodulation : modification of functional groups. Optimization receptor binding and pharmacokinetics .

Planning
Methodologies / tests Competencies Ordinary class hours Student’s personal work hours Total hours
Guest lecture / keynote speech A1 A9 A10 A13 A14 A15 A16 A21 A24 A25 B1 B2 B3 B4 B6 B7 C1 C3 C4 C6 C7 C8 16 16 32
Seminar A1 A9 A10 A13 A14 A15 A16 A21 A24 A25 B1 B2 B3 B4 B6 B7 C1 C3 C4 C6 C7 C8 7 28 35
Laboratory practice A9 A13 A14 A15 A16 A17 A18 A19 A20 A22 A23 A25 A26 B1 B2 B3 B4 B6 B7 C1 C2 C3 C4 C6 C7 C8 10 10.5 20.5
Mixed objective/subjective test A1 A9 A13 A14 A15 B2 B3 B6 C1 C6 4 20 24
 
Personalized attention 1 0 1
 
(*)The information in the planning table is for guidance only and does not take into account the heterogeneity of the students.

Methodologies
Methodologies Description
Guest lecture / keynote speech The contents will be presented. During the presentations the teacher can provide supplementary material to the literature with the aim that the explanations can be tracked effectively. The ability to create notes and search for information will also be developed.
Seminar The contents of each chapter will be discussed in seminars by solving exercises and analysis of practical cases. Students will have early enough problem sets through the Moodle platform. We may request delivery of solved exercises.
Laboratory practice Practices involving the use of software and web resources for the rational design of drugs.
Mixed objective/subjective test A test with questions related to the contents of the subject will be asked.

Personalized attention
Methodologies
Guest lecture / keynote speech
Laboratory practice
Seminar
Description
This activity will be headed to the individual assistance for explanations, doubts, as well as to the resolution of the exercises.

Part-time students and those with special academic leave permission could ask for presential or email tutorials when necessary.

Assessment
Methodologies Competencies Description Qualification
Mixed objective/subjective test A1 A9 A13 A14 A15 B2 B3 B6 C1 C6 The responses in the written exam will be evaluated. 60
Guest lecture / keynote speech A1 A9 A10 A13 A14 A15 A16 A21 A24 A25 B1 B2 B3 B4 B6 B7 C1 C3 C4 C6 C7 C8 Attendance and participation in class will be assessed 5
Laboratory practice A9 A13 A14 A15 A16 A17 A18 A19 A20 A22 A23 A25 A26 B1 B2 B3 B4 B6 B7 C1 C2 C3 C4 C6 C7 C8 Attendance and the final report will be assessed. 20
Seminar A1 A9 A10 A13 A14 A15 A16 A21 A24 A25 B1 B2 B3 B4 B6 B7 C1 C3 C4 C6 C7 C8 The active participation of students in solving the problems of the bulletins and assignment submitted will be assessed. 15
 
Assessment comments

The assistance to the lectures, seminars and practicals is mandatory.
A student can obtain the qualification of "Not presented" if do not realise activities with an upper computation to 50% in the evaluation or not to present to the mixed test.
The students will have two opportunities, and those that do not surpass the subject in the first opportunity will conserve the qualification obtained in the seminars and laboratory practicals, and will realise a second mixed test in the determinate dates by the calendar fixed by the Board of Faculty. The students that are evaluated in the second opportunity only will be able to opt to the "matrícula de honor" (highest qualification) if these have not been covered at the first opportunity.

Part-time students or students with special academic permission (according to the rules of the UDC):

The
same evaluation criteria listed above would be applied, but being not
mandatory to attend classroom lectures and seminars.

Nevertheless, It is compulsory to attend practical sessions, but  itwill be tried to fit the dates to the student's availability. When not possible otherwise,  these students should exchange the practical activities by tasks related that
not require attendance.

The
final grade will be the sum of 20% of the mark obtained in the lab practice and 80% of the mark obtained in the mixed test. The
same criteria will be applied to both opportunities.

Students who has not attended the final exam will be assessed as "non attendance".

For all the students, the education-learning process, included the evaluation, refers to an academic course and starts every new academic course, including all the activities and procedures of evaluation programed.


Sources of information
Basic Patrick, G. L (2013). An Introduction to Medicinal Chemistry. 5th ed.. New York: Oxford University Press
Avendaño, C (2001). Introducción a la Química Farmacéutica. Madrid: McGraw-Hill
Delgado, A.; Minguillón, C.; Joglar, J. (2003). Introducción a la Química Terapéutica. Madrid: Díaz de Santos
Delgado, A.; Minguillón, C.; Joglar, J. (2002). Introducción a la síntesis de fármacos. Madrid: Síntesis
Stevens, E. (2014). Medicinal Chemistry, an Introduction.. Pearson Education. New York.
Thomas, Gareth (2007). Medicinal Chemistry: An introduction. Wiley

Complementary


Recommendations
Subjects that it is recommended to have taken before
Organic Chemistry 1/610G01026
Organic Chemistry 2/610G01027
Intermediate Organic Chemistry/610G01028
Advanced Organic Chemistry/610G01030

Subjects that are recommended to be taken simultaneously
Final Dissertation/610G01043

Subjects that continue the syllabus

Other comments


(*)The teaching guide is the document in which the URV publishes the information about all its courses. It is a public document and cannot be modified. Only in exceptional cases can it be revised by the competent agent or duly revised so that it is in line with current legislation.