FAFB1_15 Medicinal Chemistry I

Farmaceutická fakulta
jaro 2021
Rozsah
3/1/0. 3 kr. Ukončení: z.
Vyučující
doc. PharmDr. Oldřich Farsa, Ph.D. (přednášející)
PharmDr. Tomáš Goněc, Ph.D. (přednášející)
Mgr. Aleš Kroutil, 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
Rozvrh
Út 8:00–10:15 44-037
  • Rozvrh seminárních/paralelních skupin:
FAFB1_15/01: Út 10:15–11:00 44-037, O. Farsa
Omezení zápisu do předmětu
Předmět je určen pouze studentům mateřských oborů.

Předmět si smí zapsat nejvýše 24 stud.
Momentální stav registrace a zápisu: zapsáno: 1/24, pouze zareg.: 0/24
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, a student will be able to know, describe, characterize or draw at least:
-main principles of general Medicinal Chemistry
-therapeutic groups presented in lectures of Medicinal Chemistry I, i.e. structures and INN names of their main representatives, their mechanisms of activity and SAR within the group
-metabolism and syntheses of selected drugs presented in seminars
Osnova
  • Medicinal Chemistry is one of five profile disciplines of pharmaceutical education. It is also a part of final state examination. Medicinal Chemistry I. covers nomenclature of drugs, their syntheses, structure-activity relationships, biotransformation and some selected approaches of drug design. It deals with a particular drug, prepared using synthetic approaches with defined structure and properties, related with its therapeutical usage in treatment of pathological states and defined diseases.
    Overwiev of lectures
  • Topic (Name of the lecturer)
    Medicinal Chemistry: Definition and history. Drug nomenclature. (Farsa)
    Physico-chemical descriptors and biological activity. Structure-Activity Relationships. Structure optimization. An introduction into Quantitative Structure-Activity Relationships (QSAR). (Farsa)
    Structure modifications: homology, analogy, isomerism, isosterism etc. (Goněc)
    Drug research and development. Drug patents. Approvals of drug preparations. Good laboratory, manufacturing and clinical practices (GLP, GMP, GCP). (Kroutil)
    Structural features influencing drug action. (Farsa)
    Adrenergic receptor agonists directly and indirectly acting. Appetite suppressants and other antiobesics. (Goněc)
    Adrenergic receptor antagonists. (Goněc)
    Drug biotransformation. Prodrugs. (Farsa)
    Weak analgesics and non-steroidal anti-inflammatory drugs (NSAIDs). Anti-osteoporotic agents. (Farsa)
    Strong analgesics - anodyns. Morphine, its derivatives and analogues. Encephalins, endorphins, opioid receptors antagonists. (Farsa)
    General and local anaesthetics. Muscle relaxants. (Farsa)
    CNS agents: antipsychotics, antineurotics. (Farsa)
    CNS agents: antidepressants, stimulants, cognitive enhancers, psychotomimetics - halucinogens. (Farsa)
    Sedatives, hypnotics. Anticonvulsants, antiepileptics. Emetics, antivomitics, antikinetics. (Farsa)
    Topics of seminars:
  • Topic (Name of the lecturer)
    *Syntheses and metabolism of selected weak analgesics and nonsteroidal anti-inflammatory drugs (NSAIDs). (Farsa)
    *Syntheses of and metabolism of selected opioid receptors´ligands. (Farsa)
    *Syntheses and metabolism of selected adrenergics and anobesics (Goněc)
    *Syntheses of platinum anticancer drugs. (Kroutil)
    *Syntheses and metabolism of selected general and local anaesthetics. (Farsa)
    *Syntheses of selected adrenergic receptor antagonists. (Goněc)
    *Syntheses and metabolism of selected antipsychotics. (Farsa)
    *Syntheses and metabolism of selected antidepressants. (Farsa)
    *Final test.
Literatura
    povinná literatura
  • Fischer János, Ganelin C. Robin. Analogue-based Drug Discovery. Weinheim, 2006. ISBN 3-527-31257-9. URL info
  • Kar Ashutosh. Medicinal Chemistry. Third edition. Tunbridge Wells, UK, 2006. info
  • M. Wolff. Burger´s Medicinal Chemistry and Drug Discovery. New York, 1994. info
    neurčeno
  • Ng Rick. Drugs: From Discovery to Approval. Second Edition. 2009. ISBN 978-0-470403587. URL info
  • Wermuth Camille Georges. The practice of Medicinal Chemistry. Third Edition. Amsterdam, 2008. info
  • Vardanyan R. S., Hruby V. J. Synthesis of Essential Drugs. Amsterdam, 2006. ISBN 978-0-444-52166-8. URL info
  • Sneader, W. Drug Discovery - A History. 2005. ISBN 9780470015520. URL info
Výukové metody
Lectures: this year on-line by MS Teams. Seminars: this year also in MS Teams.
Metody hodnocení
Written final credit test = quiz; this year on-line in Moodle.
Vyučovací jazyk
Angličtina
Další komentáře
Studijní materiály
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