aFACH2_15 Medicinal Chemistry II

Farmaceutická fakulta
jaro 2026

Předmět se v období jaro 2026 nevypisuje.

Rozsah
3/4/0. 42p+56c. 8 kr. Ukončení: zk.
Vyučující
prof. RNDr. Jozef Csöllei, CSc. (přednášející)
doc. PharmDr. Oldřich Farsa, Ph.D. (přednášející)
Mgr. Aleš Kroutil, Ph.D. (přednášející)
doc. PharmDr. Oldřich Farsa, Ph.D. (cvičící)
PharmDr. Tomáš Goněc, Ph.D. (cvičící)
RNDr. Eva Havránková, Ph.D. (cvičící)
Mgr. Petr Mokrý, Ph.D. (cvičící)
Mgr. Veronika Murgašová (cvičící)
PharmDr. Jan Otevřel, Ph.D. (cvičící)
Garance
doc. PharmDr. Oldřich Farsa, Ph.D.
Ústav chemických léčiv – Ústavy – Farmaceutická fakulta
Omezení zápisu do předmětu
Předmět je určen pouze studentům mateřských oborů.
Mateřské obory/plány
Cíle předmětu
Medicinal Chemistry (MC) is a discipline dealing mainly with relationships between chemical structure and therapeutic activity of medicines which are mostly organic but also inorganic molecules. That is why it observes the impact of physicochemical properties, space arrangement, and further structure features on the activity of a drug. It concerns in detail with mechanisms of drug interactions with target structures such as receptors´ or enzyme active sites. As a scientific discipline, MC participates importantly in the drug design and development process. As a specific discipline of the pharmaceutical study, MC is one of five stem subjects in which students do the state final exam. Here, MC can be divided into general and special parts. General MC presents general aspects of structure-activity relationships, both qualitative and quantitative, as well as common principles of derivation and proposal of structures of new medicines (analogy, homology, isomerism, isosterism...). Systematic MC deals then with the particular therapeutic groups of drugs respecting the system used in pharmacology. Here, it brings a comprehensive overview of fundamental structural types and tries to grasp the main structure-activity relationships within each group. It also reports the syntheses and metabolic pathways of some representatives of these groups. Simply said, MC builds some type of bridge between fundamental chemical disciplines, represented mainly by organic chemistry, and pharmacology.
Výstupy z učení
Every student will, after passing the subject, be capable to characterize the main groups of drugs; their main common structural characteristics if they exist; structure-activity relationships (SAR) inside narrower structural groups; their acido-basic and lipo-hydrophilic properties based on the structure; their general mechanisms of activity; particular examples of drugs in use or development from every structural group together with the exact structure or at least with main structure features in more complex molecules.
Osnova
Medicinal Chemistry II - autumn semester of the 3rd year of study
Syllabi identical with topics of particular lectures:
Lecture No. Topic Name of the lecturer)
1.Antibacterial chemotherapeutics: sulphonamides, quinolones, nitrofurans, tetracyclines. (Farsa)
2.Antibacterial chemotherapeutics continued: beta-lactam antibiotics: penicillins and cephalosporins, (poly)peptide antibiotics, aminoglycoside antibiotics, macrolide antibiotics, antibiotics of various other structures. (Farsa)
3.Tuberculostatics, leprostatics. (Farsa)
4.Antiviral agents, liver protectants. (Farsa)
5.Disinfectants, antiseptics, antiparasitics: antiprotozoal and vermicide agents, insecticides. (Farsa)
6.Diuretics, cholagogues, cholelitholytics, laxatives, antidiarrheals. (Farsa)
7.Drugs that control blood clotting. Antihyperlipidemics. (Csöllei)
8.Cardiotonics, coronary vascular dilators. Drugs improving heart perfusion. (Csöllei)
9.Anti-arrhytmics, antihypertensive agents, drugs for the treatment of erectile dysfunction. (Csöllei).
10.Drugs affecting respiratory tract: acids, antacids, anti ulcerative agents: antisecretory agents, histamine H2-receptors antagonists, H+/K+-ATPase inhibitors, gastric cytoprotectants, drugs fighting Helicobacter pylori. (Csöllei)
11.Antineoplastics. (Farsa)
12.Insulin and its analogs, synthetic antidiabetics. Hormones derived from one amino acid, thyreostatics, peptide hormones, steroid hormones, anabolic agents.
13.Biologic therapeutic agents (biologics: therapeutic monoclonal antibodies, therapeutic enzymes, antisense oligonucleotides, etc.) (Farsa)
Syllabi of practical courses
1.A short recommendation of principles of work safety and fire prevention. Sulfacetamide: synthesis, identity, confirmation by 1H-NMR.
2.Lidocaine: synthesis, identity and purity confirmation by melting point, NMR or IR spectroscopy and TLC.
3.Parabens (methyl-, ethyl-, propyl-, isopropyl- or isobutylparaben): synthesis, identity and purity confirmation by melting point and 1H-NMR spectroscopy.
4.Acetylsalicylic acid: synthesis, identity, and purity confirmation by melting point and TLC, purity by HPLC.
5.Phenytoin: synthesis, identity, and purity confirmation by melting point and/or NMR spectroscopy. Alternative: Methylthiouracil: synthesis, TLC.
6.Determination of the acid dissociation constant of nitrofurantoin or phenytoin by means of UV-VIS spectrophotometry. Final test.
7.An eventual substitute course and/or a repeated final test.
Continuous checking of study: attendance, observing of reports, and entering tests are possible.
Requirements to allow to do the exam: 100% attendance, handing-over of reports, and prepared compounds including their characterization data (melting points, chromatograms, spectra interpretaions), at least 60% success in tests.

Literatura
    doporučená literatura
  • V. Alagarsamy: Textbook of medicinal chemistry. / Volume I. Elsevier, 2010, ISBN 978-81-312-2189-1, dostupné zdarma přes https://z-lib.org/ ; též obecné kapitoly
  • V. Alagarsamy: Textbook of medicinal chemistry. / Volume II. Elsevier, 2012, ISBN: 978-81-312-2190-7, dostupné zdarma přes https://z-lib.org/
  • J. J. Li: Medicinal Chemistry for Practitioners. John Wiley & Sons Inc, 2021, ISBN 9781119607304, dostupné zdarma přes https://z-lib.org/
  • ROCHE, Victoria F.; S. William ZITO; Thomas L. LEMKE a David A. WILLIAMS. Foye's principles of medicinal chemistry. 8th edition. Philadelphia: Wolters Kluwer, 2020, xix, 1626. ISBN 9781496385024. info
  • Small molecule medicinal chemistry : strategies and technologies. Edited by Werngard Czechtizky - Peter Hamley. Hoboken, New Jersey: Wiley, 2016, 1 online. ISBN 9781118771723. URL info
  • The practice of medicinal chemistry. Edited by Camille Georges Wermuth - David Aldous - Pierre Raboisson - Didier Rog. Fourth edition. Amsterdam: Elsevier, 2015, 1 online. ISBN 9780124172135. URL info
Výukové metody
Lectures, practical lessons.
Metody hodnocení
Successfull passing of practical lessons based on full attandance, goving of products, reports and a success in final test; oral exam from the topics of lectures.
Vyučovací jazyk
Angličtina
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