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The course "Medicinal chemistry" deals with 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, receptors and nucleic acids), 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 relationships (SARs)) is discussed as well. An introduction to pharmacology is also an essential part of the course: pharmacodynamics (what the drug does to the body) and pharmacokinetics (what the body does to the drug, ADMET – absorption, distribution, metabolism, excretion, toxicity). Common classes of drugs are covered during the course (e.g. antibiotics, antivirals, anticancer agents, analgecis, etc.).
Last update: Ménová Petra (09.05.2022)
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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 structures 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. Last update: Ménová Petra (09.05.2022)
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Presentation on a given topic
Final written test
Oral exam Last update: Ménová Petra (09.05.2022)
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Graham L. Patrick: An introduction to Medicinal Chemistry, 6th edition, Oxford University Press, 2017. 978-0-19-874969-1 or Graham L. Patrick: An introduction to Medicinal Chemistry, 5th edition, Oxford University Press, 2013. 978–0–19–969739–7 PDF presentations Last update: Ménová Petra (09.05.2022)
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1. Introduction to medicinal chemistry. Definition of basic terms, drug, therapeutic index, intermolecular binding forces, drugs classification, drug development, folklore medicine. 2. Drug targets: structure and function of proteins, enzymes, receptors, and nucleic acids. Inhibitors, agonists, and antagonists. 3. Pharmacology: pharmacodynamics and pharmacokinetics, ADMET. Lipinski’s rule of 5 and its modifications. Drug metabolism. Drug administration. 4. Drug discovery, design, and development. Sources of lead compounds, evaluation of activity, SAR studies. Preclinical and clinical studies. 5. Drug delivery: technologies, prodrugs (prodrug types, ProTides), formulations. 6. Antibacterial agents: chemotherapeutics and antibiotics. Mechanisms of action, examples of drugs, drug resistence. 7. Antiviral agents. Structure and classification of viruses. Examples: influenza virus, HIV, HCV (targets, classes, and development of antivirals). 8. Anticancer agents. Cancer. Mechanisms of action, examples of drugs, drug resistance. 9. Autonomic nervous system. Cholinergic & adrenergic nervous system, receptors (nicotinic & muscarinic), neurotransmitters, SAR for acetylcholine. Acetylcholinesterase, organophosphates. 10. Pain relievers. Non-opioid analgesics and non-steroidal anti-inflammatory drugs (mechanism of action, structural classes of compounds). Opioid analgesics (mechanism of action, SAR studies). 11. Anti-ulcer agents. Stomach ulcers, Helicobacter pylori, histamine & histamine receptors, antihistamines. Binding theory for agonists & antagonists. Proton pump inhibitors. 12. Antimetabolites of nucleic acids components. Modified nucleosides with antiviral, anti-parasitic, and anticancer properties. Acyclic nucleoside phosphonates. 13. Selected case studies (anticancer, antiviral, antibiotics, analgesics). 14. Students’ presentations on selected topics (case studies).
Last update: Ménová Petra (09.05.2022)
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None Last update: Kundrát Ondřej (23.08.2018)
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None Last update: Kundrát Ondřej (23.08.2018)
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