aF1CH1_15 Medicinal Chemistry I

Faculty of Pharmacy
Autumn 2025

The course is not taught in Autumn 2025

Extent and Intensity
3/1/0. 4 credit(s). Type of Completion: z (credit).
In-person direct teaching
Teacher(s)
prof. RNDr. Jozef Csöllei, CSc. (lecturer)
doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)
Mgr. Aleš Kroutil, Ph.D. (lecturer)
doc. PharmDr. Oldřich Farsa, Ph.D. (seminar tutor)
PharmDr. Tomáš Goněc, Ph.D. (seminar tutor)
Guaranteed by
doc. PharmDr. Oldřich Farsa, Ph.D.
Department of Chemical Drugs – Departments – Faculty of Pharmacy
Course Enrolment Limitations
The course is only offered to the students of the study fields the course is directly associated with.
fields of study / plans the course is directly associated with
Course objectives
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.
Learning outcomes
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
Syllabus
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)
Literature
    recommended literature
  • DOLEŽAL, Martin. Farmaceutická chemie : léčiv působících na kardiovaskulární, trávicí a vylučovací systém. První vydání. Praha: Univerzita Karlova, vydavatelství Karolinum, 2022, 317 stran. ISBN 9788024651026. info
  • J. Hartl, K. Palát: Farmaceutická chemie I (obecná). Karolinum, Praha, 2016, ISBN 9788024620336, dostupné z e-shopu https://www.cupress.cuni.cz
  • Beneš, L., Farsa, O. Farmaceutická chemie. (Farmakochemie). Úvod do studia chemických léčiv. VFU Brno, 2005. ISBN 80-7305-516-3. info
  • 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
  • DOLEŽAL, Martin. Farmaceutická chemie léčiv působících na centrální nervový systém. Vydání 1. Praha: Karolinum, 2013, 188 stran. ISBN 9788024623825. info
  • V. Alagarsamy: Textbook of medicinal chemistry. / Volume II. Elsevier, 2012, ISBN: 978-81-312-2190-7, dostupné zdarma přes Z-Library
  • A. Borovanský, J. Csöllei. Farmaceutická chemie. Léčiva s účinkem na vegetativní nervový systém. Brno, 2004. info
  • A. Borovanský, L. Beneš. Farmaceutická chemie (Farmakochemie), Léčiva s účinkem na centrální a periferní nervový systém. Brno, 2000. info
  • A. Borovanský, J. Csőllei. Farmaceutická chemie (Farmakochemie) V. Léčiva s účinkem na respirační, gastrointestinální a vylučovací trakt. info
Teaching methods
Lectures, seminars
Assessment methods
The credit is given for at least 60 % of the credit test points.
Language of instruction
Czech
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