FaF:FAZV1_15 Molecular Principles of Drug D - Course Information

FAZV1_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-FARMA)

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)
  February15th Introduction into the discipline, its concept and organisation. Combinatorial chemistry as a tool of drug design. (Farsa)
  February 22nd Physico-chemical properties of compounds and their importance for the activity in the organism. (Goněc)
  March 1st Quantitative structure-activity relationships (Farsa)
  March 8th Optimisation of physico-chemical properties based on analogy. (Goněc)
  March 15th Design of strong analgesics. (Zubáč)
  March 22nd Development of biologic therapeutics. (Farsa)
  March 29th Theory of priviledged structures. Chemogenomics. (Hudcová)
  April 5th Fragment method in drug design. (Václavík)
  April 12th Design of drugs with respect to their metabolism I. Toxic metabolites. (Goněc)
  April 19th Design of drugs with respect to their metabolism II. Prodrugs and their design. (Goněc)
  April 26th Development of specific veterinary medicines. (Zubáč)
  May 3rd Membrane transporters and their importance for drug design. (Goněc)
  May 10th Efflux pumps and their importance in drug design and development. (Zubáč)
  May 17th Interaction of a target structure and a drug on molecular level. (Goněc)
  Brno, February 14th, 2018

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
• Kubinyi H., Müller G. Chemogenomics in Drug Discovery: A Medicinal Chemistry Perspective. 2004. ISBN 9783527603947. info

not specified
• Sneader, W. Drug Discovery - A History. 2005. ISBN 9780470015520. URL info

Teaching methods (in Czech)

Přednášení
Laborování

Assessment methods (in Czech)

Známkou
Písemná zkouška

Language of instruction

English

Further comments (probably available only in Czech)

Study Materials
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 performed in the form of a written test.

• Enrolment Statistics (Spring 2020, recent)
  
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