FACL1_15 Basics of Chemical Drugs

Faculty of Pharmacy
Spring 2020
Extent and Intensity
2/1/0. 4 credit(s). Type of Completion: zk (examination).
Teacher(s)
prof. RNDr. Jozef Csöllei, CSc. (lecturer)
Mgr. Petr Mokrý, Ph.D. (lecturer)
PharmDr. Pavlína Marvanová, Ph.D. (seminar tutor)
Mgr. Petr Mokrý, Ph.D. (seminar tutor)
PharmDr. Tereza Padrtová, Ph.D. (seminar tutor)
Guaranteed by
Mgr. Petr Mokrý, Ph.D.
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
Course objectives
The aim of this subject is to offer the students, in connection with the Medicinal Chemistry, known common information about the chemical structure, which is responsible for chemical and physico-chemical properties and forms the basis for biological action.
The program of the lectures is constituted of nomenclature principles of synthetic drugs, structural factors influencing the biological activity of drugs and modification of their structure using the principles of isomerism, homology and analogy. The separate part is represented by the lectures about selected active fragments and heterocyclic compounds occurring in several pharmacological groups.
The seminar part offers the overview of synthetic reactions leading to the formation of selected compounds, used as drugs or their intermediates.
Syllabus
  • - Definition and characterization of the subject
    - Nomenclature of organic compounds, nomenclature principles of synthetic drugs
    - Structural factors influencing the biological activity of drugs
    - Drug structure modifications using the principles of isomerism, homology and analogy
    - Active fragments occurring in several pharmacological groups
    - Heterocyclic compounds occurring in several pharmacological groups
    - Carbon-carbon bond forming reactions (Friedel-Crafts reactions, alkylation of active hydrogen compounds, Gattermann reaction, Grignard reaction, Wurtz-Fittig reaction, halogenalkylation (chloromethylation), Kolbe-Schmitt reaction)
    - Carbon-hydrogen bond forming reactions (reduction of multiple bonds carbon-carbon, dehalogenation, dehydroxylation, deamination, decarboxylation, desulfonylation)
    - Carbon-halogen bond forming reactions (substitution reactions - halogenation of alkanes, cycloalkanes and aromatic compounds, addition reaction of carbon-carbon multiple bonds)
    - Carbon-oxygen bond forming reactions (preparation of alcohols, phenols, ethers, carbonyl compounds and carboxylic acids)
    - Carbon-nitrogen bond forming reactions (preparation of amines, nitro compounds, amides, nitriles, hydrazides)
Literature
    required literature
  • MCMURRY, John. Organic chemistry. 8th ed. Belmont: Brooks/Cole, 2012. ISBN 978-0-8400-5444-9. info
  • R.S. Vardanyan and V.J. Hruby. Synthesis of Essential Drugs. Elsevier, 2006. ISBN 978-0-444-52166-8. info
    recommended literature
  • János Fischer, C. Robin Ganellin. Analogue-based Drug Discovery. Wiley-VCH Verlag GmbH & Co. KGaA, 2006. ISBN 9783527608003. info
  • Mukund S. Chorghade. Drug Discovery and Development, Volume 1. John Wiley & Sons, Inc., 2006. ISBN 9780470320778. info
Language of instruction
English
Further comments (probably available only in Czech)
The course can also be completed outside the examination period.
Teacher's information
- students are required 100% attendance at seminars
- credit test (at least 60 % of the points)
- written exam
  • Enrolment Statistics (recent)
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