aFACH1_15 Medicinal Chemistry I

Farmaceutická fakulta
podzim 2025

Předmět se v období podzim 2025 nevypisuje.

Rozsah
3/1/0. 42p+14s. 4 kr. Ukončení: z.
Vyučující
prof. RNDr. Jozef Csöllei, CSc. (přednášející)
doc. PharmDr. Oldřich Farsa, Ph.D. (přednášející)
doc. PharmDr. Oldřich Farsa, Ph.D. (cvičící)
PharmDr. Tomáš Goněc, Ph.D. (cvičící)
Mgr. Aleš Kroutil, 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 physico-chemical properties, space arrangement and further structure features on the activity of a drug. It concerns in detail with mechanisms of drug intearactions 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 pharmacetical 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 qulitative 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 overwiev of fundamental structural types and tries to grasp main structure-activity relationships within each group. It also reports syntheses and methabolic 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
After passing the subject, students will have to know, explain, present or draw as follows: -main principles of general Medicinal Chemistry
-therapeutic groups presented in seminars, ie. INN names and structures of main representatives, fundamental structure-activity relationships (SAR), brief mechanism of action
-basics of metabolism and synthesis in therateutic groups, for which this was presented in seminars
-an interpretation of NMR and IR spektra of a drug or other simple organic molecule, including its standardized listing, as required for practical classes in Medicinal Chemistry II in the following semester
Osnova
Medicinal Chemistry is one of five profile disciplines of pharmaceutical education. It is also a part of the final state examination. Medicinal Chemistry I. covers the nomenclature of drugs, their syntheses, structure-activity relationships, biotransformation and some selected approaches of drug design. It deals with a drug, prepared using synthetic approaches with defined structure and properties, related with its therapeutical usage in the treatment of pathological states and defined diseases.
Topics of lectures (lecturers: doc. PharmDr. Oldřich Farsa, PhD., PharmDr. Tomáš Goněc, Mgr. Aleš Kroutil)
Medicinal Chemistry: Definition and history. Drug nomenclature.(Farsa)
Drugs research and development. Drug patents. Approvals of drug preparations. Good laboratory, manufacturing and clinical practices (GLP, GMP, GCP). (Kroutil)
Structure modifications: homology, analogy, isomerism, isosterism etc. (Goněc)
Physico-chemical descriptors and biological activity. Structure-activity relationships. Structure optimization. Quantitative structure-activity relationships (QSAR).(Farsa)
Structural factors influencing drug action. (Farsa)
Drugs biotransformation. Prodrugs.
Weak analgesics and non-steroidal antiinflammatory drugs (NSAIDs). Anti-osteoporotic agents.(Farsa)
General and local anesthetics. Myorelaxants. (Farsa)
Strong analgesics - anodyns. Morphine and its derivatives. Encephalins, endorphins, opioid receptors antagonists. (Farsa)
CNS agents: antidepressants, stimulants, cognitive enhancers, psychotomimetics - hallucinogens.(dr. Farsa)
CNS agents: antipsychotics, antineurotics.(Farsa)
Sedatives, hypnotics. Anticonvulsans, antiepileptics. Emetics, antivomitics, antikinetics. (Farsa)
Adrenergic receptor agonists directly and indirectly acting. Appetite suppressants and other antiobesics. (Goněc)
Adrenergic receptor antagonists. (Goněc)
Literatura
    doporučená literatura
  • V. Alagarsamy: Textbook of medicinal chemistry. / Volume II. Elsevier, 2012, ISBN: 978-81-312-2190-7, dostupné zdarma přes Z-Library
  • V. Alagarsamy: Textbook of medicinal chemistry. / Volume I. Elsevier, 2010, ISBN 978-81-312-2189-1, dostupné přes https://z-lib.org/ nebo pomocí Z-Library pro mobily ; též obecné kapitoly
  • Náhradní obsah: 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, seminars
Metody hodnocení
The credit is given for at least 60 % of the credit test points.
Vyučovací jazyk
Angličtina
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