FaF:FAFB1_15 Medicinal Chemistry I - Course Information

FAFB1_15 Medicinal Chemistry I

Extent and Intensity

3/1/0. 3 credit(s). Type of Completion: z (credit).

Teacher(s)

doc. PharmDr. Oldřich Farsa, Ph.D. (lecturer)
PharmDr. Tomáš Goněc, Ph.D. (lecturer)
Mgr. Aleš Kroutil, Ph.D. (lecturer)
doc. PharmDr. Oldřich Farsa, Ph.D. (seminar tutor)
PharmDr. Tomáš Goněc, Ph.D. (seminar tutor)
Mgr. Aleš Kroutil, Ph.D. (seminar tutor)

Guaranteed by

Department of Chemical Drugs – Departments – Faculty of Pharmacy

Course Enrolment Limitations

The course is also offered to the students of the fields other than those the course is directly associated with.

fields of study / plans the course is directly associated with

• Pharmacy (programme FaF, M-FARMA)

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.

Syllabus

• 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.
  Timetable of lectures (lecturers: doc. PharmDr. Oldřich Farsa, PhD., PharmDr. Tomáš Goněc, PhD., Mgr. Aleš Kroutil)
  Date Topic (Name of the lecturer)
  February 18th Medicinal Chemistry: Definition and history. Drug nomenclature. (Farsa)
  February 25th Physico-chemical descriptors and biological activity. Structure-Activity Relationships. Structure optimization. An introduction into Quantitative Structure-Activity Relationships (QSAR). (Farsa)
  March 3rd Structure modifications: homology, analogy, isomerism, isosterism etc. (Goněc)
  March 10th Drugs research and development. Drug patents. Approvals of drug preparations. Good laboratory, manufacturing and clinical practices (GLP, GMP, GCP). (Kroutil)
  March 17th Structural features influencing drug action. (Farsa)
  March 24th Adrenergic receptor agonists directly and indirectly acting. Appetite suppressants and other antiobesics. (Goněc)
  March 31st Adrenergic receptor antagonists. (Goněc)
  April 7th Drugs biotransformation. Prodrugs. (Farsa)
  April 14th Weak analgesics and non-steroidal anti-inflammatory drugs (NSAIDs). Anti-osteoporotic agents. (Farsa)
  April 21st Strong analgesics - anodyns. Morphine, its derivatives and analogues. Encephalins, endorphins, opioid receptors antagonists. (Farsa)
  April 28th General and local anaesthetics. Muscle relaxants. (Farsa)
  May 5th CNS agents: antipsychotics, antineurotics. (Farsa)
  May 12th CNS agents: antidepressants, stimulants, cognitive enhancers, psychotomimetics - halucinogens. (Farsa)
  May 19th 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.

Literature

required literature
• 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

not specified
• 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

Teaching methods (in Czech)

Přednášení
Monologická (výklad, přednáška, instruktáž)
Dialogická (diskuze, rozhovor, brainstorming)

Assessment methods (in Czech)

Písemná zkouška

Language of instruction

English

Further Comments

Study Materials
The course can also be completed outside the examination period.

Teacher's information

Elementary knowledge of drug stuctures and structure-activity relationships in every particular therapeutical group.

• Enrolment Statistics (Spring 2020, recent)
  
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