F1FB1_15 Medicinal Chemistry I

Faculty of Pharmacy
Spring 2022
Extent and Intensity
3/1/0. 3 credit(s). Type of Completion: z (credit).
Taught in person.
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
Supplier department: Department of Chemical Drugs – Departments – Faculty of Pharmacy
Timetable
Thu 8:00–9:15 44–056, Thu 11:25–12:40 44–056
  • Timetable of Seminar Groups:
F1FB1_15/01: each odd Friday 7:30–9:10 44–037, T. Goněc
F1FB1_15/02: each odd Friday 9:25–11:05 44–037, T. Goněc
F1FB1_15/03: each even Friday 7:30–9:10 44–037, O. Farsa
F1FB1_15/04: each even Friday 9:25–11:05 44–037, T. Goněc
Course Enrolment Limitations
The course is also offered to the students of the fields other than those the course is directly associated with.
The capacity limit for the course is 160 student(s).
Current registration and enrolment status: enrolled: 94/160, only registered: 0/160, only registered with preference (fields directly associated with the programme): 0/160
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
-the same for groups presented in seminars
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.
    Timetable of lectures (lecturers: doc. PharmDr. Oldřich Farsa, PhD., PharmDr. Tomáš Goněc, Mgr. Aleš Kroutil)
    February 22nd Medicinal Chemistry: Definition and history. Drug nomenclature.(Farsa)
    March 1st Drugs research and development. Drug patents. Approvals of drug preparations. Good laboratory, manufacturing and clinical practices (GLP, GMP, GCP). (Kroutil)
    March 8th Structure modifications: homology, analogy, isomerism, isosterism etc. (Goněc)
    March 15th Physico-chemical descriptors and biological activity. Structure-activity relationships. Structure optimization. Quantitative structure-activity relationships (QSAR).(Farsa)
    March 22nd Structural factors influencing drug action. (Farsa)
    March 19th Drugs biotransformation. Prodrugs.
    April 5th Weak analgesics and non-steroidal antiinflammatory drugs (NSAIDs). Anti-osteoporotic agents.(Farsa)
    April 12th General and local anesthetics. Myorelaxants. (Farsa)
    April 19th Strong analgesics - anodyns. Morphine and its derivatives. Encephalins, endorphins, opioid receptors antagonists. (Farsa)
    April 26th CNS agents: antidepressants, stimulants, cognitive enhancers, psychotomimetics - hallucinogens.(dr. Farsa)
    May 3rd CNS agents: antipsychotics, antineurotics.(Farsa)
    May 10th Sedatives, hypnotics. Anticonvulsans, antiepileptics. Emetics, antivomitics, antikinetics. (Farsa)
    May 17th Adrenergic receptor agonists directly and indirectly acting. Appetite suppressants and other antiobesics. (Goněc)
    May 24th Adrenergic receptor antagonists. (Goněc)
Literature
    required literature
  • M. Wolff. Burger´s Medicinal Chemistry and Drug Discovery. New York, 1994. info
Teaching methods
Classical lectures in a lecture hall. Seminars with your own presentations in the seminar room 44-037.
Assessment methods
The credit is given for a satisfactory point evaluation of the seminar's presentation and at least 60 % of the credit test points.
Language of instruction
Czech
Further comments (probably available only in Czech)
Study Materials
The course can also be completed outside the examination period.
Listed among pre-requisites of other courses
The course is also listed under the following terms Spring 2020, Spring 2021, Spring 2023, Spring 2024, Spring 2025.
  • Enrolment Statistics (Spring 2022, recent)
  • Permalink: https://is.muni.cz/course/pharm/spring2022/F1FB1_15