COURSE OBJECTIVE
To acquaint students with the importance of synthetic organic chemistry in drug development, and the division of drugs according to selected therapeutic groups and to support examples of the synthesis of effective and selective compounds with pharmacological effects.
COURSE IMPLEMENTATION PROGRAM
WEEK 1
Introduction to a rational approach to drug design.
Definitions and goals of medical chemistry research.
Receptors and drug action.
Strategies for finding lead compounds.
Relationship structure and activity (SAR).
WEEK 2
Targets of action of drugs, enzymes.
Enzyme substrates as drugs, enzyme inhibitors as drugs, enzyme regulation.
WEEK 3
Drug development strategies: natural compounds; development of new drugs.
Rational approach to drug design, bioisosteria in drug development, application of prodrugs.
WEEK 4
General and local anesthetics: division, modes of action, mechanism of action, examples.
WEEK 5
Sedatives and hypnotics: division (barbiturates and non-barbiturates), modes and mechanism of action, breakdown of barbiturates, structure-activity ratio (SAR), benzodiazepine synthesis.
WEEK 6
Anticonvulsants and muscle relaxants: division, modes of action, mechanism of action, chemotherapy of epilepsy, muscle neuroblockers.
WEEK 7
Antipyretic and narcotic analgesics: division, mechanism of action, salicylic acid derivatives, quinoline derivatives, characteristics and limitations of opiate analgesics, morphine analogues.
WEEK 8
Cardiovascular drugs: mechanism of action, cardiac glycosides, antihypertensives, antiarrhythmics, vasodilators.
WEEK 9
Antihistamines: division, causative factors of allergic diseases, mechanism of action of antihistamines, histamine H1 receptor antagonists, histamine H2 receptor blockers.
WEEK 10
Nonsteroidal anti-inflammatory drugs (NSAIDs): division, mechanism of action, derivatives of heteroaryloacetic, aryl-propionic and salicylic acids, gold compounds.
WEEK 11
Sulfonamides: division; mechanism of action, sulfonamides for general, urinary and intestinal infections, bacterial resistance to sulfonamide drugs.
WEEK 12
Anthelmintics and antimalarials: division, mechanism of action, quinoline, guanidine, pyrimidine, piperazine, benzimidazole analogs, natural compounds.
WEEK 13
Antibiotics: division, beta-lactames, aminoglycoside and quinolone antibiotics, tetracyclines, SAR.
WEEK 14
Antitumor drugs: division, mechanism of action, alkylating agents, DNA intercalators, photodynamic therapy, protein kinase inhibitors, topoisomerase inhibitors, microtubule and tubulin inhibitors.
WEEK 15
Antiviral drugs: division, replication and transformation, compounds that inhibit the early stage of virus replication, compounds that interfere with viral nucleic acid replication, mechanisms of action.
DEVELOPING GENERAL AND SPECIFIC COMPETENCIES OF STUDENTS
Enabling students to solve the problem of synthesis of target molecules with pharmacological effects in research and development laboratories of pharmaceutical companies and research institutes.
STUDENT OBLIGATIONS IN TEACHING AND THEIR PERFORMANCE
Students are required to attend lectures.
Students are required to do all the lab exercises.
Students are required to access knowledge tests and colloquia (related to laboratory exercises).
CONDITIONS FOR OBTAINING SIGNATURES
80% attendance at lectures.
Completed laboratory exercises and passed the final colloquium in laboratory exercises.
TEACHING METHODS
Lectures (ex cathedra)
Lecture through e-learning
Laboratory exercises (practical work in groups under the supervision of an assistant)
Consultations by arrangement with students
MANNER OF EXAMINATION OF KNOWLEDGE AND EXAMINATION
Colloquium from laboratory exercises.
2 mandatory written partial tests during the semester (60% of points on each of the tests brings exemption from the oral exam).
Written exam (requires 50% points to pass).
Oral exam.
METHOD OF MONITORING THE QUALITY AND PERFORMANCE OF COURSES
Student survey.
METHODOLOGICAL PREREQUISITES
COURSE LEARNING OUTCOMES
1. to apply complex principles related to medicinal chemistry and rational approach in drug design
2. to identify some of the targets of drug action and apply basic knowledge of organic chemistry and biochemistry in understanding the structure and mechanisms of biological action of basic groups of drugs
3. to analyze the targets of drug action and apply basic strategies of medicinal chemistry in the development of pharmacologically active compounds
4. to use a modern laboratory methods and procedures in the synthesis of potential biologically active compounds, and analyze and present the obtained results
5. to interpret and present certain types of drugs from selected therapeutic groups
LEARNING OUTCOMES AT PROGRAM LEVEL
1. to connect a basic facts, concepts, chemical principles and theories related to advanced areas of chemistry and chemical technologies
2. to apply more complex chemical principles that continue the basic knowledge of chemistry acquired in undergraduate study
3. to demonstrate the ability to work independently with minimal mentoring
4. to use advanced laboratory procedures and instrumentation within chemical synthesis and analysis
5. to plan independently experiments with self-criticism in the evaluation of experimental procedures and results
TEACHING UNITS WITH ASSOCIATED LEARNING OUTCOMES AND EVALUATION CRITERIA
Teaching unit
1. Rational approach and strategies of medicinal chemistry in drug design
Learning outcomes
- to define research objectives in medical chemistry and strategies for finding leading compounds
- to apply strategies in a rational approach to drug design (bioisosteria, prodrugs)
- to identify and define the main targets of drug action
- to interpret the function and importance of enzymes
Evaluation criteria
- to understand a rational approach to drug design
- to determine research objectives in medicinal chemistry and strategy for finding lead compounds and SAR
- to understand the differences in the mechanisms of action between individual therapeutic groups of drugs
- to understand the function and importance of enzymes
- to understand the function of prodrugs
2. Classification of drugs according to selected therapeutic groups , Antiviral drugs)
Learning outcomes
- to list, identify and interpret the types of drugs, their production, and ways and mechanisms of their biological action
- to classify drugs according to selected therapeutic groups
- to analyze the mechanisms of biological action of a particular type of drug
- to synthesize selected representatives of drugs by modern synthetic methods, and to analyze, interpret and present the obtained results
Evaluation criteria
- to know the types of drugs and the ways and mechanisms of their biological action
- to know the types of drugs according to the selected therapeutic groups
- to understand the mechanisms of biological action of a particular type of drug
- to plan the synthesis of selected drug representatives
|
-
MEDICINAL CHEMISTRY, R. B. Silverman, M. Holladay, The Organic Chemistry of Drug Design and Drug Action, Third Edition, Elsevier, 2015.
D. Lednicer, STRATEGIES FOR ORGANIC DRUG SYNTHESIS AND DESIGN, John Wiley and Sons, New Jersey, 2009., A. Kar, New Age International (P) Ltd. Publisher New Delhi., 2007.
-
MEDICINSKA KEMIJA, J. R. Hanson, CHEMISTRY AND MEDICINES, RSC Publishing, Cambridge, 2006.
R. R. Nadendla, PRINCIPLES OF ORGANIC MEDICINAL CHEMISTRY, New Age International, New Delhi, 2005., M. Mintas, S. Raić-Malić, Medicinska naklada, Zagreb, 2009.
|
Pristupačnost
