FaF:F1ZV1_15 Molecular Principles of Drug D - Course Information

F1ZV1_15 Molecular Principles of Drug Design

Extent and Intensity

2/1/0. 4 credit(s). Type of Completion: zk (examination).

Teacher(s)

doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)
PharmDr. Tomáš Goněc, Ph.D. (lecturer)
doc. PharmDr. Oldřich Farsa, Ph.D. (seminar tutor)
PharmDr. Tomáš Goněc, Ph.D. (seminar tutor)

Guaranteed by

Department of Chemical Drugs – Departments – Faculty of Pharmacy

Course Enrolment Limitations

The course is also offered to the students of the fields other than those the course is directly associated with.

fields of study / plans the course is directly associated with

• Pharmacy (programme FaF, M-FARM)

Course objectives

Objectives of the course:
The course develops and deepens knowledge of pharmaceutical chemistry in combination with other pharmaceutical and biological branches of knowledge in terms of drug research and development strategy. The key objective is structure proposal and further optimisations so that a new potential drug met basic bioavailability requirements, i.e. absorption, distribution, and binding to receptors.

Content:
The course covers knowledge at the interface between pharmaceutical chemistry, pharmacology, molecular biology and pharmaceutical technology. Approaches generally used at drug structure development, including QSAR, combinatorial chemistry, molecular modelling, and fragment approach are discussed. Structural factors affecting biological effect, factors affecting drug absorption and transport to the place of action, and drug binding to receptors are considered. Polymorphism, influence of particle size, and other physico-chemical methods of drug molecule modification are regarded. The review of actual administrative regulations in the sphere of drug development is provided.

Syllabus

• Lecturers: doc. PharmDr. Oldřich Farsa, Ph.D., PharmDr. Tomáš Goněc, Ph.D., Mgr. Anna Hudcová, Mgr. Jiří Václavík, Ph.D., Mgr. Peter Zubáč
  Topics of lectures (Thursday 9.30 11.00)
  1. Introduction into the discipline, its concept and organisation. Combinatorial chemistry as a tool of drug design. (Farsa)
  2. Physico-chemical properties of compounds and their importance for the activity in the organism. (Goněc)
  3. Quantitative structure-activity relationships (Farsa)
  4. Optimisation of physico-chemical properties based on analogy. (Goněc)
  5. Design of strong analgesics. (Zubáč)
  6. Development of biologic therapeutics. (Farsa)
  7. Theory of priviledged structures. Chemogenomics. (Hudcová)
  8. Fragment method in drug design. (Václavík)
  9. Design of drugs with respect to their metabolism I. Toxic metabolites. (Goněc)
  10. Design of drugs with respect to their metabolism II. Prodrugs and their design. (Goněc)
  11. Development of specific veterinary medicines. (Zubáč)
  12. Membrane transporters and their importance for drug design. (Goněc)
  13. Efflux pumps and their importance in drug design and development. (Zubáč)
  14. Interaction of a target structure and a drug on molecular level. (Goněc)
  

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 (in Czech)

Přednášení
Laborování

Assessment methods (in Czech)

Známkou
Písemná zkouška

Language of instruction

Czech

Further comments (probably available only in Czech)

The course can also be completed outside the examination period.

Teacher's information

Students will obtain credit after participation in all lectures. The examination is realized in the form of the written test.

• Enrolment Statistics (Spring 2020, recent)
  
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