SubjectsSubjects(version: 855)
Course, academic year 2019/2020
  
Medicinal Chemistry - P110015
Title: Medicinální chemie
Guaranteed by: Department of Organic Chemistry (110)
Actual: from 2019
Semester: winter
Points: winter s.:0
E-Credits: winter s.:0
Examination process: winter s.:
Hours per week, examination: winter s.:3/0 other [hours/week]
Capacity: unknown / unknown (unknown)
Min. number of students: unlimited
Language: English
Teaching methods: full-time
Level:  
For type: doctoral
Note: can be fulfilled in the future
Guarantor: Janeba Zlatko Ing. Ph.D.
Interchangeability : AP110015
Is interchangeable with: AP110015
Annotation -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)
The "Medicinal chemistry" course deals with the drug discovery, design and development. Attention is paid to the description of the mechanism of action of drugs, to interactions of drugs with their molecular targets (e.g. enzymes and receptors), and to the study of physico-chemical properties of compounds. The relationship between biological properties (activity) of the compounds and their chemical structure (structure-activity relationship (SAR) study) is discussed as well. During the course, common classes of drugs (e.g. antibiotics, antivirals, anticancer agents) and the basics of pharmacodynamics (what the drug does to the body) and pharmacokinetics (what the body does to the drug), including ADMET (absorption, distribution, metabolism, excretion, toxicity) are also discussed. An excursion to IOCB (medicinal chemistry, virology, biochemical pharmacology) will also be part of the course.
Aim of the course -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

Students will learn what medicinal chemistry is, and what drugs and their molecular targets (enzymes, receptors, etc.) are. They will understand the principles of pharmacodynamics and pharmacokinetics. They will learn about key drug classes, such as antibiotics, antivirals, anticancer agents, analgesics, and anti-inflammatory agents. They will know how the structure of a potential drugs are designed and optimized, how the biological properties of compounds can be improved, and they will understand the process of preclinical development of drugs.

Literature -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

B: Graham L. Patrick: An introduction to Medicinal Chemistry, 5th edition, Oxford University Press, 2013. 978–0–19–969739–7

R: Wermuth G. Camille (Ed.): The Practice of Medicinal Chemistry, 3rd edition, Elsevier AP, 2008. 978–0–12–374194–3

R: Silverman B. Richard: The Organic Chemistry of Drug Design and Drug Action, 2nd edition, Elsevier AP, 2004. 978–0–12–643732–4

R: Nencka Radim: Základní principy výzkumu nových léčiv, 1. vydání, Univerzita Palackého v Olomouci, 2015. 978-80-244-4538-0 (in Czech only)

Syllabus -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

1. What is medicinal chemistry, definition of basic terms. Drugs

2. Drug targets: structure of proteins, enzymes, receptors, and nucleic acids

3. Pharmacodynamics and pharmacokinetics (including ADMET)

4. Drug discovery, design, and development. Hit, lead, optimization, SAR studies

5. Tools and computers in medicinal chemistry, combinatorial and parallel synthesis, HTS, biological assays

6. Antibacterial agents (bacteria, classes, targets, drug resistance)

7. Antiviral agents (viruses, classes, targets, drug resistance)

8. Anticancer agents (cancer, targets, resistance)

9. Cholinergics, anticholinergics, and anticholinesterases. Adrenergic receptors, agonists and antagonists

10. Opioid analgesics, anti-inflammatory agents, NSAID

11. Anti-ulcer agents. Antidepressant agents

12. Drug delivery (technologies, prodrugs, formulations)

13. Selected case studies (anticancer, antiviral, antibiotics, analgesics)

14. Students’ presentations on selected topics (case studies)

Entry requirements -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

None

Registration requirements -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

None

Course completion requirements -
Last update: Kundrát Ondřej Ing. Ph.D. (23.08.2018)

Presentation on given topic

Final written test

Oral exam

 
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