FaF:FDCZV_FAF Molecular Bases of Drug Deve - Course Information

FDCZV_FAF Molecular Bases of Drug Development

Extent and Intensity

1/1/0. 15 credit(s). Type of Completion: zk (examination).

Teacher(s)

doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)

Guaranteed by

doc. PharmDr. Oldřich Farsa, Ph.D.
Faculty of Pharmacy

Prerequisites (in Czech)

FAKULTA(FaF)

Course Enrolment Limitations

The course is only offered to the students of the study fields the course is directly associated with.

fields of study / plans the course is directly associated with

• Medicinal Chemistry (programme FaF, D-FCH) (2)

Course objectives

A specific drug molecule is in the spotlight of this discipline. The advanced course proceeds the general Medicinal Chemistry and develops it towards research and development of medicines on molecular level. The discipline sums up different approaches and protocols either typical only for Medicinal Chemistry (priviledged structures´ concept, drug likeness, pharmacogenomics, fragment method, molecular docking etc.) or adapted from other more general disciplines (QSAR including physico-chemical descriptors used there, combinatorial chemistry). The discipline touches also methods of the acitity assessment of biologicaly active compounds in vitro, some pharmacokinetic systems (efflux pumps) and specifity of development of veterinary drugs. The development in some model therapeutic groups is here described in more detail (strong analgesics as an example of small moleculs, haematopoietic factors as an example of biologic therapeutics).

Learning outcomes

The knowledge of the topics of the discipline to the extent which will be preliminarily agreed among the guarantor, Ph.D. student and his/her tutor.

Syllabus

• 
  Topics
  1. Introduction into the discipline, its concept and organisation. Combinatorial chemistry as a tool of drug design.
  2. Physico-chemical properties of compounds and their importance for the activity in the organism.
  3. Quantitative structure-activity relationships.
  4. Optimisation of physico-chemical properties based on analogy.
  5. Design of strong analgesics.
  6. Development of biologic therapeutics.
  7. Theory of priviledged structures. Chemogenomics.
  8. Fragment method in drug design.
  9. Design of drugs with respect to their metabolism I. Toxic metabolites.
  10. Design of drugs with respect to their metabolism II. Prodrugs and their design.
  11. Development of specific veterinary medicines.
  12. Membrane transporters and their importance for drug design.
  13. Efflux pumps and their importance in drug design and development. (
  14. Interaction of a target structure and a drug on molecular level.
  

Literature

recommended literature
• Avdeef, A. Absorption and Drug Development. info
• Fischer, J., Ganellin, C.R. Analogue-based Drug Discovery. ISBN 978-3-572-31257-3. info
• You, G.F., Morris, M.E. Drug Transporters. ISBN 978-0-471-78491-3. info
• Pliška, V., Testa, B., van de Waterbeemd, H. Lipophilicity in Drug Action and Toxicology. ISBN 3-527-29383-3. info
• Hilficker, R. Polymorphism. ISBN 978-3-527-31146-0. info
• Kerns, E.H., Di, L. Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization. 2008. ISBN 978-0-1236-9520-8. info
• Kubinyi, H. QSAR: Hansch Analysis and Related Approaches. 2008. ISBN 9783527616824. URL info
• Wermuth, C.G. The Practice of Medicinal Chemistry, 3rd. Edition. 2008. ISBN 978-0-12-374194-3. info
• Beneš, L., Farsa, O. Farmaceutická chemie. (Farmakochemie). Úvod do studia chemických léčiv. VFU Brno, 2005. ISBN 80-7305-516-3. info
• Kubinyi H., Müller G. Chemogenomics in Drug Discovery: A Medicinal Chemistry Perspective. 2004. ISBN 9783527603947. info
• Hartl, J., Palát, K. Farmaceutická chemie I. Karolinum, Praha, 1998. ISBN 80-7184-619-8. info
• Kuchař M., Rejholec V. Využití kvantitativních vztahů mezi strukturou a biologickou aktivitou. Academia,. Praha, 1987. info

Teaching methods

Self-study of resources recommended by the subject guarantor to the extent agreed between the subject guarantor, the DSP student and his tutor.

Assessment methods

With a mark
Oral exam

Language of instruction

Czech

Further Comments

Study Materials
The course can also be completed outside the examination period.
The course is taught each semester.

• Enrolment Statistics (Autumn 2020, recent)
  
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